A topical medication is a
medication
A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy (pharmacotherapy) is an important part of the medical field and re ...
that is applied to a particular place on or in the body. Most often topical medication means application to
body surfaces such as the
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
or
mucous membrane
A mucous membrane or mucosa is a membrane that lines various cavities in the body of an organism and covers the surface of internal organs. It consists of one or more layers of epithelial cells overlying a layer of loose connective tissue. It is ...
s to treat ailments via a large range of classes including
creams,
foams
Foams are materials formed by trapping pockets of gas in a liquid or solid.
A bath sponge and the head on a glass of beer are examples of foams. In most foams, the volume of gas is large, with thin films of liquid or solid separating the reg ...
,
gels
A gel is a semi-solid that can have properties ranging from soft and weak to hard and tough. Gels are defined as a substantially dilute cross-linked system, which exhibits no flow when in the steady-state, although the liquid phase may still di ...
,
lotions
Lotion is a low-viscosity topical preparation intended for application to the skin. By contrast, creams and gels have higher viscosity, typically due to lower water content. Lotions are applied to external skin with bare hands, a brush, a clean ...
, and ointments.
Many topical medications are epicutaneous, meaning that they are applied directly to the skin. Topical medications may also be
inhalational
Inhalation (or Inspiration) happens when air or other gases enter the lungs.
Inhalation of air
Inhalation of air, as part of the cycle of breathing, is a vital process for all human life. The process is autonomic (though there are exceptions ...
, such as
asthma medication
Asthma is a long-term inflammatory disease of the airways of the lungs. It is characterized by variable and recurring symptoms, reversible airflow obstruction, and easily triggered bronchospasms. Symptoms include episodes of wheezing, cou ...
s, or applied to the surface of tissues other than the skin, such as
eye drops
Eye drops or eyedrops are liquid drops applied directly to the surface of the eye usually in small amounts such as a single drop or a few drops. Eye drops usually contain saline to match the salinity of the eye. Drops containing only saline ...
applied to the
conjunctiva
The conjunctiva is a thin mucous membrane that lines the inside of the eyelids and covers the sclera (the white of the eye). It is composed of non-keratinized, stratified squamous epithelium with goblet cells, stratified columnar epithelium ...
, or
ear drop
Ear drops are a form of topical medication for the ears used to treat otitis, infection, inflammation, Earwax#Excess earwax (impacted cerumen), impacted ear wax and local anesthesia. They are commonly used for short-term treatment and can be pur ...
s placed in the ear, or medications applied to the surface of a
tooth
A tooth ( : teeth) is a hard, calcified structure found in the jaws (or mouths) of many vertebrates and used to break down food. Some animals, particularly carnivores and omnivores, also use teeth to help with capturing or wounding prey, tear ...
. The word ''topical'' derives from
Greek
Greek may refer to:
Greece
Anything of, from, or related to Greece, a country in Southern Europe:
*Greeks, an ethnic group.
*Greek language, a branch of the Indo-European language family.
**Proto-Greek language, the assumed last common ancestor ...
τοπικός ''topikos'', "of a place".
Justification
Topical drug delivery Topical drug delivery (TDD) is a route of drug administration that allows the topical formulation to be delivered across the skin upon application, hence producing a localized effect to treat skin disorders like eczema. The formulation of topical d ...
is a route of administering
drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insuffla ...
s via the
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
to provide topical therapeutic effects. As
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
is one of the largest and most superficial
organs
In biology, an organ is a collection of tissues joined in a structural unit to serve a common function. In the hierarchy of life, an organ lies between tissue and an organ system. Tissues are formed from same type cells to act together in a fu ...
in the
human
Humans (''Homo sapiens'') are the most abundant and widespread species of primate, characterized by bipedalism and exceptional cognitive skills due to a large and complex brain. This has enabled the development of advanced tools, culture, ...
body,
pharmacist
A pharmacist, also known as a chemist (Commonwealth English) or a druggist (North American and, archaically, Commonwealth English), is a healthcare professional who prepares, controls and distributes medicines and provides advice and instructi ...
s utilise it to deliver various drugs. This system usually provides a local effect on certain positions of the body. In ancient times, people used
herb
In general use, herbs are a widely distributed and widespread group of plants, excluding vegetables and other plants consumed for macronutrients, with savory or aromatic properties that are used for flavoring and garnishing food, for medicinal ...
s to put on wounds for relieving the inflammatory effect or as pain relievers. The use of
topical drug
A topical medication is a medication that is applied to a particular place on or in the body. Most often topical medication means application to body surfaces such as the skin or mucous membranes to treat ailments via a large range of classes ...
delivery system is much broader now, from
smoking cessation
Smoking cessation, usually called quitting smoking or stopping smoking, is the process of discontinuing tobacco smoking. Tobacco smoke contains nicotine, which is addictive and can cause dependence. As a result, nicotine withdrawal often make ...
to beauty purposes. Nowadays, there are numerous
dosage form
Dosage forms (also called unit doses) are pharmaceutical drug products in the form in which they are marketed for use, with a specific mixture of active ingredients and inactive components (excipients), in a particular configuration (such as a cap ...
s that can be used topically, including
cream
Cream is a dairy product composed of the higher-fat layer skimmed from the top of milk before homogenization. In un-homogenized milk, the fat, which is less dense, eventually rises to the top. In the industrial production of cream, this process ...
,
ointment
A topical medication is a medication that is applied to a particular place on or in the body. Most often topical medication means application to body surfaces such as the skin or mucous membranes to treat ailments via a large range of classes ...
,
lotion
Lotion is a low-viscosity topical preparation intended for application to the skin. By contrast, creams and gels have higher viscosity, typically due to lower water content. Lotions are applied to external skin with bare hands, a brush, a clean ...
,
patches, dusting powder and much more. There are many advantages for this
drug delivery system - avoiding
first pass metabolism
The first pass effect (also known as first-pass metabolism or presystemic metabolism) is a phenomenon of drug metabolism whereby the concentration of a drug, specifically when administered orally, is greatly reduced before it reaches the system ...
which can increase its
bioavailability
In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation.
By definition, when a medication is administered intravenously, its bioavailability is 100%. H ...
, being convenient and easy to apply to a large area, being easy to terminate the medication and avoiding gastro-intestinal irritations. All these can increase the patient compliance. However, there are several disadvantages for this system - causing
skin irritation
Irritation, in biology and physiology, is a state of inflammation or painful reaction to allergy or cell-lining damage. A stimulus or agent which induces the state of irritation is an irritant. Irritants are typically thought of as chemical age ...
s and symptoms like
rash
A rash is a change of the human skin which affects its color, appearance, or texture.
A rash may be localized in one part of the body, or affect all the skin. Rashes may cause the skin to change color, itch, become warm, bumpy, chapped, dry, cr ...
es and
itchiness
Itch (also known as pruritus) is a sensation that causes the desire or reflex to scratch. Itch has resisted many attempts to be classified as any one type of sensory experience. Itch has many similarities to pain, and while both are unpleasant ...
may occur. Also, only small
particle
In the Outline of physical science, physical sciences, a particle (or corpuscule in older texts) is a small wikt:local, localized physical body, object which can be described by several physical property, physical or chemical property, chemical ...
s can pass through the
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
, which limits the choice of
drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insuffla ...
s. Since
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
is the main medium of topical drug delivery system, its conditions determine the rate of skin penetration leading to affecting the
pharmacokinetics
Pharmacokinetics (from Ancient Greek ''pharmakon'' "drug" and ''kinetikos'' "moving, putting in motion"; see chemical kinetics), sometimes abbreviated as PK, is a branch of pharmacology dedicated to determining the fate of substances administered ...
of the
drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insuffla ...
. The
temperature
Temperature is a physical quantity that expresses quantitatively the perceptions of hotness and coldness. Temperature is measured with a thermometer.
Thermometers are calibrated in various temperature scales that historically have relied o ...
,
pH value
In chemistry, pH (), historically denoting "potential of hydrogen" (or "power of hydrogen"), is a scale used to specify the acidity or basicity of an aqueous solution. Acidic solutions (solutions with higher concentrations of ions) are mea ...
and dryness of the
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
need to be considered. There are some novel topical drugs in the market which can utilise the system as much as possible.
This localized system provides topical therapeutic effects via
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
,
eye
Eyes are organs of the visual system. They provide living organisms with vision, the ability to receive and process visual detail, as well as enabling several photo response functions that are independent of vision. Eyes detect light and conv ...
s,
nose
A nose is a protuberance in vertebrates that houses the nostrils, or nares, which receive and expel air for respiration alongside the mouth. Behind the nose are the olfactory mucosa and the sinuses. Behind the nasal cavity, air next passes th ...
and
vagina
In mammals, the vagina is the elastic, muscular part of the female genital tract. In humans, it extends from the vestibule to the cervix. The outer vaginal opening is normally partly covered by a thin layer of mucosal tissue called the hymen ...
to treat
iseases The most common usage is for local
skin infection
A skin infection is an infection of the skin in humans and other animals, that can also affect the associated soft tissues such as loose connective tissue and mucous membranes. They comprise a category of infections termed skin and skin structure ...
problems. Dermatological products have various
formulations
Formulation is a term used in various senses in various applications, both the material and the abstract or formal. Its fundamental meaning is the putting together of components in appropriate relationships or structures, according to a formul ...
and range in consistency though the most popular dermal products are semisolid dosage forms to provide topical treatment.
Factor affecting topical drug absorption
Topical drug absorption depends on two major factors - biological and physicochemical properties.
The first factor concerns body structure effects on the
drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insuffla ...
s. The degradation of drugs can be affected by the site of applications. Some studies discovered different
Percutaneous {{More citations needed, date=January 2021
In surgery, a percutaneous procedurei.e. Granger et al., 2012 is any medical procedure or method where access to inner organs or other tissue is done via needle-puncture of the skin, rather than by using ...
absorption patterns. Apart from the place, age also affects the absorption as the skin structure changes with age. The lowered
collagen
Collagen () is the main structural protein in the extracellular matrix found in the body's various connective tissues. As the main component of connective tissue, it is the most abundant protein in mammals, making up from 25% to 35% of the whole ...
and broadened
blood capillary
A capillary is a small blood vessel from 5 to 10 micrometres (μm) in diameter. Capillaries are composed of only the tunica intima, consisting of a thin wall of simple squamous endothelial cells. They are the smallest blood vessels in the body: ...
networks happen with ageing. These features alter the effectiveness of absorption of both hydrophilic and
lipophilic substance
Lipophilicity (from Greek language, Greek λίπος "fat" and :wikt:φίλος, φίλος "friendly"), refers to the ability of a chemical compound to dissolve in fats, oils, lipids, and non-polar solvents such as hexane or toluene. Such non-pol ...
s into
stratum
In geology and related fields, a stratum ( : strata) is a layer of rock or sediment characterized by certain lithologic properties or attributes that distinguish it from adjacent layers from which it is separated by visible surfaces known as ei ...
corneum underneath the surface of skin. The skin surface integrity can also affect the permeability of drugs such as the density of
hair follicle
The hair follicle is an organ found in mammalian skin. It resides in the dermal layer of the skin and is made up of 20 different cell types, each with distinct functions. The hair follicle regulates hair growth via a complex interaction between h ...
s,
sweat gland
Sweat glands, also known as sudoriferous or sudoriparous glands, , are small tubular structures of the skin that produce sweat. Sweat glands are a type of exocrine gland, which are glands that produce and secrete substances onto an epithelial sur ...
s or disintegrated by
inflammation
Inflammation (from la, wikt:en:inflammatio#Latin, inflammatio) is part of the complex biological response of body tissues to harmful stimuli, such as pathogens, damaged cells, or Irritation, irritants, and is a protective response involving im ...
or
dehydration
In physiology, dehydration is a lack of total body water, with an accompanying disruption of metabolic processes. It occurs when free water loss exceeds free water intake, usually due to exercise, disease, or high environmental temperature. Mil ...
.
The other factor concerns metabolism of medications on
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
. When the percutaneous drug is applied on
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
, it will be gradually absorbed down the
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
. Normally, when the drugs are absorbed, they will be metabolised by various
enzyme
Enzymes () are proteins that act as biological catalysts by accelerating chemical reactions. The molecules upon which enzymes may act are called substrates, and the enzyme converts the substrates into different molecules known as products. A ...
s in our body and the amount will be lower. The exact amount delivered to the target action site determines the potency and bioavailability of the drugs. If the
concentration
In chemistry, concentration is the abundance of a constituent divided by the total volume of a mixture. Several types of mathematical description can be distinguished: '' mass concentration'', ''molar concentration'', ''number concentration'', an ...
is too low, the therapeutic effect is impeded; if the concentration is too high, drug toxicity may happen to cause side effects or even do harm to our body. For the
topical drug
A topical medication is a medication that is applied to a particular place on or in the body. Most often topical medication means application to body surfaces such as the skin or mucous membranes to treat ailments via a large range of classes ...
delivery way, degradation of drugs in skin is very low compared to
liver
The liver is a major Organ (anatomy), organ only found in vertebrates which performs many essential biological functions such as detoxification of the organism, and the Protein biosynthesis, synthesis of proteins and biochemicals necessary for ...
. The metabolism of drugs is mainly by metabolic enzyme
cytochrome P450
Cytochromes P450 (CYPs) are a Protein superfamily, superfamily of enzymes containing heme as a cofactor (biochemistry), cofactor that functions as monooxygenases. In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are ...
, and this enzyme is not active in skin. The
CYP450
Cytochromes P450 (CYPs) are a superfamily of enzymes containing heme as a cofactor that functions as monooxygenases. In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are important for the clearance of various compo ...
actively metabolized drugs can then maintain high concentration when being applied on skin. Despite
CYP450
Cytochromes P450 (CYPs) are a superfamily of enzymes containing heme as a cofactor that functions as monooxygenases. In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are important for the clearance of various compo ...
enzyme action, the
partition coefficient
In the physical sciences, a partition coefficient (''P'') or distribution coefficient (''D'') is the ratio of concentrations of a compound in a mixture of two immiscible solvents at equilibrium. This ratio is therefore a comparison of the solub ...
(K) determines the activity of topical drugs. The ability of drug particles to go through the skin layer also affects the absorption of drugs. For transdermal activity, medicines with higher K value are harder to get rid of the
lipid layer of skin cells. The trapped molecules then cannot penetrate into the skin. This reduces the efficacy of the transdermal drugs. The drugs target cells underneath the
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
or need to diffuse into
blood capillary
A capillary is a small blood vessel from 5 to 10 micrometres (μm) in diameter. Capillaries are composed of only the tunica intima, consisting of a thin wall of simple squamous endothelial cells. They are the smallest blood vessels in the body: ...
to exert their effect. Meanwhile, the size of particles affects this transdermal process. The smaller the drug molecules, the faster the rate of penetration.
Polarity
Polarity may refer to:
Science
*Electrical polarity, direction of electrical current
*Polarity (mutual inductance), the relationship between components such as transformer windings
* Polarity (projective geometry), in mathematics, a duality of ord ...
of the drugs can affect this diffusion rate too. If the drug shows lower degree of ionization, it is less polar. Therefore, it can have a faster absorption rate.
Local versus systemic effect
The definition of the topical
route of administration
A route of administration in pharmacology and toxicology is the way by which a medication, drug, fluid, poison, or other substance is taken into the body.
Routes of administration are generally classified by the location at which the substance i ...
sometimes states that both the application location and the
pharmacodynamic
Pharmacodynamics (PD) is the study of the biochemical and physiologic effects of drugs (especially pharmaceutical drugs). The effects can include those manifested within animals (including humans), microorganisms, or combinations of organisms (for ...
effect thereof is local.
In other cases, ''topical'' is defined as applied to a localized area of the body or to the surface of a body part regardless of the location of the effect. By this definition, topical administration also includes
transdermal
Transdermal is a route of administration wherein active ingredients are delivered across the skin for systemic distribution. Examples include transdermal patches used for medicine delivery.
The drug is administered in the form of a patch or ointme ...
application, where the substance is administered onto the skin but is
absorbed into the body to attain
systemic
Systemic fundamental to a predominant social, economic, or political practice. This refers to:
In medicine
In medicine, ''systemic'' means affecting the whole body, or at least multiple organ systems. It is in contrast with ''topical'' or ''loc ...
distribution. Such medications are generally
hydrophobic
In chemistry, hydrophobicity is the physical property of a molecule that is seemingly repelled from a mass of water (known as a hydrophobe). In contrast, hydrophiles are attracted to water.
Hydrophobic molecules tend to be nonpolar and, th ...
chemicals, such as
steroid hormone
A steroid hormone is a steroid that acts as a hormone. Steroid hormones can be grouped into two classes: corticosteroids (typically made in the adrenal cortex, hence ''cortico-'') and sex steroids (typically made in the gonads or placenta). Wi ...
s. Specific types include
transdermal patch
A transdermal patch is a medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream. An advantage of a transdermal drug delivery route over other types of medicat ...
es which have become a popular means of administering some drugs for
birth control
Birth control, also known as contraception, anticonception, and fertility control, is the use of methods or devices to prevent unwanted pregnancy. Birth control has been used since ancient times, but effective and safe methods of birth contr ...
,
hormone replacement therapy
Hormone replacement therapy (HRT), also known as menopausal hormone therapy or postmenopausal hormone therapy, is a form of hormone therapy used to treat symptoms associated with female menopause. These symptoms can include hot flashes, vaginal ...
, and prevention of
motion sickness
Motion sickness occurs due to a difference between actual and expected motion. Symptoms commonly include nausea, vomiting, cold sweat, headache, dizziness, tiredness, loss of appetite, and increased salivation. Complications may rarely include d ...
. One example of an
antibiotic
An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting bacterial infections, and antibiotic medications are widely used in the treatment and prevention of ...
that may be applied topically is
chloramphenicol
Chloramphenicol is an antibiotic useful for the treatment of a number of bacterial infections. This includes use as an eye ointment to treat conjunctivitis. By mouth or by injection into a vein, it is used to treat meningitis, plague, cholera, a ...
.
If defined strictly as having local effect, the topical
route of administration
A route of administration in pharmacology and toxicology is the way by which a medication, drug, fluid, poison, or other substance is taken into the body.
Routes of administration are generally classified by the location at which the substance i ...
can also include
enteral administration
Enteral administration is food or drug administration via the human gastrointestinal tract. This contrasts with parenteral nutrition or drug administration (Greek ''para'', "besides" + ''enteros''), which occurs from routes outside the GI tract ...
of medications that are poorly absorbable by the
gastrointestinal tract
The gastrointestinal tract (GI tract, digestive tract, alimentary canal) is the tract or passageway of the digestive system that leads from the mouth to the anus. The GI tract contains all the major organ (biology), organs of the digestive syste ...
. One poorly absorbable antibiotic is
vancomycin
Vancomycin is a glycopeptide antibiotic medication used to treat a number of bacterial infections. It is recommended intravenously as a treatment for complicated skin infections, bloodstream infections, endocarditis, bone and joint infections, ...
, which is recommended by mouth as a treatment for severe
''Clostridium difficile'' colitis.
Choice of base formulation
A medication's potency often is changed with its base. For example, some
topical steroid Topical steroids are the topical forms of corticosteroids. Topical steroids are the most commonly prescribed topical medications for the treatment of rash, eczema, and dermatitis. Topical steroids have anti-inflammatory properties and are classifie ...
s will be classified one or two strengths higher when moving from cream to ointment. As a rule of thumb, an ointment base is more occlusive and will drive the medication into the skin more rapidly than a solution or cream base.
[Wolverton, SE. ''Comprehensive Dermatologic Drug Therapy.'' WB Saunders. 2001. pp 563-572.]
The manufacturer of each topical product has total control over the content of the base of a medication. Although containing the same active ingredients, one manufacturer's cream might be more acidic than the next, which could cause skin irritation or change its absorption rate. For example, a vaginal formulation of
miconazole
Miconazole, sold under the brand name Monistat among others, is an antifungal medication used to treat ring worm, pityriasis versicolor, and yeast infections of the skin or vagina. It is used for ring worm of the body, groin (jock itch), and fee ...
antifungal cream might irritate the skin less than an athlete foot formulation of miconazole cream. These variations can, on occasion, result in different
clinical outcome
Clinical endpoints or clinical outcomes are outcome measures referring to occurrence of disease, symptom, sign or laboratory abnormality constituting a target outcome in clinical research trials. The term may also refer to any disease or sign t ...
s, even though the active ingredient is the same. No comparative potency labeling exists to ensure equal efficacy between brands of topical steroids (percentage of oil vs water dramatically affect the potency of topical steroid). Studies have confirmed that the potency of some topical steroid products may differ according to manufacturer or brand. An example of this is the case of brand name
Valisone
Betamethasone is a corticosteroid, steroid medication. It is used for a number of diseases including rheumatic disorders such as rheumatoid arthritis and systemic lupus erythematosus, skin diseases such as dermatitis and psoriasis, allergic con ...
cream and
Kenalog cream in clinical studies have demonstrated significantly better vasoconstrictions than some forms of this drug produced by
generic drug
A generic drug is a pharmaceutical drug that contains the same chemical substance as a drug that was originally protected by chemical patents. Generic drugs are allowed for sale after the patents on the original drugs expire. Because the active ch ...
manufacturers.
However, in a simple base like an ointment, much less variation between manufacturers is common.
In
dermatology
Dermatology is the branch of medicine dealing with the skin.''Random House Webster's Unabridged Dictionary.'' Random House, Inc. 2001. Page 537. . It is a speciality with both medical and surgical aspects. A dermatologist is a specialist medical ...
, the base of a topical medication is often as important as the medication itself. It is extremely important to receive a medication in the correct base, before applying to the skin. A pharmacist should not substitute an ointment for a cream, or vice versa, as the potency of the medication can change. Some physicians use a thick ointment to replace the waterproof barrier of the inflamed skin in the treatment of eczema, and a cream might not accomplish the same clinical intention.
Formulations
There are many general classes, with no clear dividing line among similar formulations. As a result, what the manufacturer's marketing department chooses to list on the label of a topical medication might be completely different from what the form would normally be called.
Cream
A
cream
Cream is a dairy product composed of the higher-fat layer skimmed from the top of milk before homogenization. In un-homogenized milk, the fat, which is less dense, eventually rises to the top. In the industrial production of cream, this process ...
is an emulsion of oil and water in approximately equal proportions. It penetrates the
stratum corneum
The stratum corneum (Latin for 'horny layer') is the outermost layer of the epidermis. The human stratum corneum comprises several levels of flattened corneocytes that are divided into two layers: the ''stratum disjunctum'' and ''stratum compact ...
outer layer of skin wall. Cream is thicker than lotion, and maintains its shape when removed from its container. It tends to be moderate in moisturizing tendency. For topical steroid products, oil-in-water emulsions are common. Creams have a significant risk of causing
immunological sensitization In immunology, the term sensitization is used for the following concepts:Anderson DM, ed. (2003). "Sensitization." ''Dorland's Illustrated Medical Dictionary'', 30th ed. Philadelphia: Saunders, p. 1680. .Brown MJ, ed. (1992). "Sensitization." ''Mill ...
due to
preservative
A preservative is a substance or a chemical that is added to products such as food products, beverages, pharmaceutical drugs, paints, biological samples, cosmetics, wood, and many other products to prevent decomposition by microbial growth or by ...
s and have a high rate of acceptance by patients. There is a great variation in ingredients, composition, pH, and tolerance among generic brands.
Foam
Foam
Foams are materials formed by trapping pockets of gas in a liquid or solid.
A bath sponge and the head on a glass of beer are examples of foams. In most foams, the volume of gas is large, with thin films of liquid or solid separating the reg ...
can be seen with topical steroid marketed for the scalp.
Gel
Gel
A gel is a semi-solid that can have properties ranging from soft and weak to hard and tough. Gels are defined as a substantially dilute cross-linked system, which exhibits no flow when in the steady-state, although the liquid phase may still di ...
s are thicker than liquids. Gels are often a semisolid
emulsion
An emulsion is a mixture of two or more liquids that are normally immiscible (unmixable or unblendable) owing to liquid-liquid phase separation. Emulsions are part of a more general class of two-phase systems of matter called colloids. Althoug ...
and sometimes use alcohol as a solvent for the active ingredient; some gels liquefy at body temperature. Gel tends to be cellulose cut with alcohol or acetone. Gels tend to be self-drying, tend to have greatly variable ingredients between brands, and carry a significant risk of inducing hypersensitivity due to fragrances and preservatives. Gel is useful for hairy areas and body folds. In applying gel one should avoid fissures in the skin, due to the stinging effect of the alcohol base. Gel enjoys a high rate of acceptance due to its cosmetic elegance.
Lotion
Lotion
Lotion is a low-viscosity topical preparation intended for application to the skin. By contrast, creams and gels have higher viscosity, typically due to lower water content. Lotions are applied to external skin with bare hands, a brush, a clean ...
s are similar to solution but are thicker and tend to be more
emollient
A moisturizer, or emollient, is a cosmetic preparation used for protecting, moisturizing, and lubricating the skin. These functions are normally performed by sebum produced by healthy skin. The word "emollient" is derived from the Latin verb ''mo ...
in nature than solution. They are usually oil mixed with water, and more often than not have less alcohol than solution. Lotions can be drying if they contain a high amount of alcohol.
Ointment
An ointment is a homogeneous, viscous, semi-solid preparation, most commonly a greasy, thick oil (oil 80% - water 20%) with a high viscosity, that is intended for external application to the skin or mucous membranes. Ointments have a
water number
A topical medication is a medication that is applied to a particular place on or in the body. Most often topical medication means application to body surfaces such as the skin or mucous membranes to treat ailments via a large range of classes ...
that defines the maximum amount of water that they can contain. They are used as
emollient
A moisturizer, or emollient, is a cosmetic preparation used for protecting, moisturizing, and lubricating the skin. These functions are normally performed by sebum produced by healthy skin. The word "emollient" is derived from the Latin verb ''mo ...
s or for the application of active ingredients to the skin for protective, therapeutic, or prophylactic purposes and where a degree of occlusion is desired.
Ointments are used topically on a variety of body surfaces. These include the
skin
Skin is the layer of usually soft, flexible outer tissue covering the body of a vertebrate animal, with three main functions: protection, regulation, and sensation.
Other cuticle, animal coverings, such as the arthropod exoskeleton, have diffe ...
and the
mucous membrane
A mucous membrane or mucosa is a membrane that lines various cavities in the body of an organism and covers the surface of internal organs. It consists of one or more layers of epithelial cells overlying a layer of loose connective tissue. It is ...
s of the
eye
Eyes are organs of the visual system. They provide living organisms with vision, the ability to receive and process visual detail, as well as enabling several photo response functions that are independent of vision. Eyes detect light and conv ...
(an ''eye ointment''),
chest
The thorax or chest is a part of the anatomy of humans, mammals, and other tetrapod animals located between the neck and the abdomen. In insects, crustaceans, and the extinct trilobites, the thorax is one of the three main divisions of the crea ...
,
vulva
The vulva (plural: vulvas or vulvae; derived from Latin for wrapper or covering) consists of the external sex organ, female sex organs. The vulva includes the mons pubis (or mons veneris), labia majora, labia minora, clitoris, bulb of vestibu ...
,
anus
The anus (Latin, 'ring' or 'circle') is an opening at the opposite end of an animal's digestive tract from the mouth. Its function is to control the expulsion of feces, the residual semi-solid waste that remains after food digestion, which, d ...
, and
nose
A nose is a protuberance in vertebrates that houses the nostrils, or nares, which receive and expel air for respiration alongside the mouth. Behind the nose are the olfactory mucosa and the sinuses. Behind the nasal cavity, air next passes th ...
. An ointment may or may not be medicated.
Ointments are usually very moisturizing, and good for dry skin. They have a low risk of sensitization due to having few ingredients beyond the base oil or fat, and low irritation risk. There is typically little variability between brands of drugs. They are often disliked by patients due to greasiness.
The vehicle of an ointment is known as the ''ointment base''. The choice of a base depends upon the clinical indication for the ointment. The different types of ointment bases are:
* Absorption bases, e.g.,
beeswax
Beeswax (''cera alba'') is a natural wax produced by honey bees of the genus ''Apis''. The wax is formed into scales by eight wax-producing glands in the abdominal segments of worker bees, which discard it in or at the hive. The hive workers ...
and
wool fat
Lanolin (from Latin 'wool', and 'oil'), also called wool yolk, wool wax, or wool grease, is a wax secreted by the sebaceous glands of wool-bearing animals. Lanolin used by humans comes from domestic sheep breeds that are raised specifically fo ...
* Emulsifying bases, e.g.,
cetrimide
Cetrimide, or alkyltrimethylammonium bromide, is an antiseptic which is a mixture of three quaternary ammonium compounds: tetradonium bromide (TTAB or MITMAB), cetrimonium bromide (CTAB), and laurtrimonium bromide (DTAB or LTAB). It was first di ...
and
emulsifying wax Emulsifying wax is a cosmetic emulsifying ingredient. The ingredient name is often followed by the initials NF, indicating that it conforms to the specifications of the National Formulary.
Emulsifying wax is created when a wax material (either a ve ...
* Hydrocarbon bases, e.g.,
ceresine
Ceresin (also cerin, cerasin, cerosin, ceresin wax or ceresine) is a wax derived from ozokerite by a purifying process.
The purifying process of the ozokerite commonly comprises a treatment with heat and sulfuric acid, but other processes are a ...
,
microcrystalline wax
Microcrystalline waxes are a type of wax produced by de-oiling petrolatum, as part of the petroleum refining process. In contrast to the more familiar paraffin wax which contains mostly unbranched alkanes, microcrystalline wax contains a higher per ...
,
hard paraffin, and
soft paraffin
* Vegetable oil bases, e.g.,
almond oil
The almond (''Prunus amygdalus'', syn. ''Prunus dulcis'') is a species of tree native to Iran and surrounding countries, including the Levant. The almond is also the name of the edible and widely cultivated seed of this tree. Within the genus ...
,
coconut oil
frameless , right , alt = A cracked coconut and a bottle of coconut oil
Coconut oil (or coconut butter) is an edible oil derived from the wick, meat, and milk of the coconut palm fruit. Coconut oil is a white solid fat; in warmer climates duri ...
,
olive oil
Olive oil is a liquid fat obtained from olives (the fruit of ''Olea europaea''; family Oleaceae), a traditional tree crop of the Mediterranean Basin, produced by pressing whole olives and extracting the oil. It is commonly used in cooking: f ...
,
peanut oil
Peanut oil, also known as groundnut oil or arachis oil, is a vegetable oil derived from peanuts. The oil usually has a mild or neutral flavor but, if made with roasted peanuts, has a stronger peanut flavor and aroma. It is often used in American ...
, and
sesame oil
Sesame oil is an edible vegetable oil derived from sesame seeds. The oil is one of the earliest-known crop-based oils. Worldwide mass modern production is limited due to the inefficient manual harvesting process required to extract the oil. O ...
* Water-soluble bases, e.g.,
macrogol
Macrogol, also known as polyethylene glycol (PEG), is used as a medication to treat constipation in children and adults. It is also used to empty the bowels before a colonoscopy. It is taken by mouth. Benefits usually occur within three days. ...
s 200, 300, 400
The medicaments are dispersed in the base and are divided after penetrating the living cells of the skin.
The water number of an ointment is the maximum quantity of water that 100g of a base can contain at 20 °C.
Ointments are formulated using hydrophobic, hydrophilic, or water-emulsifying bases to provide preparations that are immiscible, miscible, or emulsifiable with skin secretions. They can also be derived from hydrocarbon (fatty), absorption, water-removable, or water-soluble bases.
Evaluation of ointments:
# Drug content
# Release of medicament from base
# Medicament penetration
# Consistency of the preparation
# Absorption of medicament into blood stream
# Irritant effect
Properties which affect choice of an ointment base are:
# Stability
# Penetrability
# Solvent property
# Irritant effects
# Ease of application and removal
Methods of preparation of ointments:
* Fusion: In this method the ingredients are melted together in descending order of their melting points and stirred to ensure homogeneity.
* Trituration: In this finely subdivided insoluble medicaments are evenly distributed by grinding with a small amount of the base followed by dilution with gradually increasing amounts of the base.
Paste
Paste combines three agents - oil, water, and powder. It is an ointment in which a powder is suspended.
Powder
Powder
A powder is a dry, bulk solid composed of many very fine particles that may flow freely when shaken or tilted. Powders are a special sub-class of granular materials, although the terms ''powder'' and ''granular'' are sometimes used to distin ...
is either the pure drug by itself (talcum powder), or is made of the drug mixed in a carrier such as
corn starch
Corn starch, maize starch, or cornflour (British English) is the starch derived from corn (maize) grain. The starch is obtained from the endosperm of the kernel. Corn starch is a common food ingredient, often used to thicken sauces or sou ...
or corn cob powder (Zeosorb AF - miconazole powder). Can be used as an inhaled topical (
cocaine
Cocaine (from , from , ultimately from Quechuan languages, Quechua: ''kúka'') is a central nervous system (CNS) stimulant mainly recreational drug use, used recreationally for its euphoria, euphoric effects. It is primarily obtained from t ...
powder used in nasal surgery).
Shake lotion
A shake lotion is a mixture that separates into two or three parts over time. Frequently, an oil mixed with a water-based solution needs to be shaken into suspension before use and includes the instructions: "Shake well before use".
Solid
Medication may be placed in a solid form. Examples are deodorant, antiperspirants, astringents, and hemostatic agents. Some solids melt when they reach body temperature (e.g. rectal suppositories).
Sponge
Certain contraceptive methods rely on
sponge
Sponges, the members of the phylum Porifera (; meaning 'pore bearer'), are a basal animal clade as a sister of the diploblasts. They are multicellular organisms that have bodies full of pores and channels allowing water to circulate through t ...
as a carrier of a liquid medicine.
Lemon juice
The lemon (''Citrus limon'') is a species of small evergreen trees in the flowering plant family Rutaceae, native to Asia, primarily Northeast India (Assam), Northern Myanmar or China.
The tree's ellipsoidal yellow fruit is used for culina ...
embedded in a sponge has been used as a primitive contraception in some cultures.
Tape
Cordran tape is an example of a topical steroid applied under
occlusion
Occlusion may refer to:
Health and fitness
* Occlusion (dentistry), the manner in which the upper and lower teeth come together when the mouth is closed
* Occlusion miliaria, a skin condition
* Occlusive dressing, an air- and water-tight trauma ...
by tape. This greatly increases the potency and absorption of the topical steroid and is used to treat inflammatory skin diseases.
Tincture
A
tincture
A tincture is typically an extract of plant or animal material dissolved in ethanol (ethyl alcohol). Solvent concentrations of 25–60% are common, but may run as high as 90%.Groot Handboek Geneeskrachtige Planten by Geert Verhelst In chemistr ...
is a skin preparation that has a high percentage of alcohol. It would normally be used as a drug vehicle if drying of the area is desired.
Topical solution
Topical solutions can be marketed as drops, rinses, or sprays, are generally of low viscosity, and often use alcohol or water in the base. These are usually a powder dissolved in alcohol, water, and sometimes oil; although a solution that uses alcohol as a base ingredient, as in topical steroids, can cause drying of the skin.
[Alt URL]
/ref> There is significant variability among brands, and some solutions may cause irritation, depending on the preservative(s) and fragrances used in the base.
Some examples of topical solutions are given below:
# Aluminium acetate topical solution: This is colorless, with a faint acetous odour and sweetish taste. It is applied topically as an astringent after dilution with 10-40 parts of water. This is used in many types of dermatologic creams, lotions, and pastes. Commercial premeasured and packed tablets and powders are available for this preparation.
# Povidone iodine topical solution: This is a chemical complex of iodine with polyvinylpyrrolidone. The agent is a polymer with an average molecular weight of 40,000. The povidone iodine contains 10% available iodine, slowly released when applied to skin. This preparation is employed topically as a surgical scrub and non irritating antiseptic solution; its effectiveness is directly attributed to the presence and release of iodine from the complex. Commercial product: Betadine
Povidone-iodine (PVP-I), also known as iodopovidone, is an antiseptic used for skin disinfection before and after surgery. It may be used both to disinfect the hands of healthcare providers and the skin of the person they are caring for. It may a ...
solution.
Transdermal patch
Transdermal patch
A transdermal patch is a medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream. An advantage of a transdermal drug delivery route over other types of medicat ...
es can be a very precise time released method of delivering a drug. Cutting a patch in half might affect the dose delivered. The release of the active component from a transdermal delivery system (patch) may be controlled by diffusion through the adhesive which covers the whole patch, by diffusion through a membrane which may only have adhesive on the patch rim or drug release may be controlled by release from a polymer matrix. Cutting a patch might cause rapid dehydration of the base of the medicine and affect the rate of diffusion.
Vapor
Some medications are applied as an ointment or gel, and reach the mucous membrane via vaporization. Examples are nasal topical decongestant Topical decongestants are decongestants applied directly to the nasal cavity. Their effectiveness by themselves in the common cold appears to have a small benefit in adults.
Topical decongestants should only be used by patients for a maximum of 5 ...
s and smelling salt.
Topical Drug Classification System (TCS)
Topical drug classification system (TCS) is proposed by the FDA
The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food s ...
. It is designed from the Biopharmaceutics Classification System
The Biopharmaceutics Classification System is a system to differentiate the drugs on the basis of their solubility and permeability.
This system restricts the prediction using the parameters solubility and intestinal permeability. The solubility ...
(BCS) for oral immediate release solid drug products which is very successful for decades. There are 3 aspects to assess and 4 classes in total. The 3 aspects include qualitative (Q1), quantitative (Q2) and similarity of in vitro
''In vitro'' (meaning in glass, or ''in the glass'') studies are performed with microorganisms, cells, or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in biology an ...
release (IVR) rate (Q3).
Advantages of topical drug delivery systems
In the early 1970s, the Alza Corporation
Alza Corporation was a pharmaceutical and medical systems company.
Background
Founded in 1968 by Dr. Alejandro Zaffaroni; the company's name is a portmanteau of his name. Alza was a major pioneer in the field of drug delivery systems, bringing ...
, through their founder Alejandro Zaffaroni
Alejandro Zaffaroni (February 27, 1923 – March 1, 2014) was a Uruguayan serial entrepreneur who was responsible for founding several biotechnology companies in Silicon Valley. Products that he was involved in developing include the birth contro ...
, filed the first US patents describing transdermal delivery systems for scopolamine
Scopolamine, also known as hyoscine, or Devil's Breath, is a natural or synthetically produced tropane alkaloid and anticholinergic drug that is formally used as a medication for treating motion sickness and postoperative nausea and vomiting ...
, nitroglycerin
Nitroglycerin (NG), (alternative spelling of nitroglycerine) also known as trinitroglycerin (TNG), nitro, glyceryl trinitrate (GTN), or 1,2,3-trinitroxypropane, is a dense, colorless, oily, explosive liquid most commonly produced by nitrating g ...
and nicotine
Nicotine is a natural product, naturally produced alkaloid in the nightshade family of plants (most predominantly in tobacco and ''Duboisia hopwoodii'') and is widely used recreational drug use, recreationally as a stimulant and anxiolytic. As ...
. People found that applying medicines on the body surfaces is beneficial in many aspects. Skin medicines can give faster onset and local effect on our body as the surface cream can bypass first pass metabolism such as hepatic and intestinal metabolism. Apart from the absorption, dermal drugs effectively prevent oral delivery limitations such as nausea
Nausea is a diffuse sensation of unease and discomfort, sometimes perceived as an urge to vomit. While not painful, it can be a debilitating symptom if prolonged and has been described as placing discomfort on the chest, abdomen, or back of the ...
and vomiting
Vomiting (also known as emesis and throwing up) is the involuntary, forceful expulsion of the contents of one's stomach through the mouth and sometimes the Human nose, nose.
Vomiting can be the result of ailments like Food-poisoning, foo ...
and poor appliances due to unpalatable tastes of the drugs . Topical application is an easy way for patients to tackle skin infections in a painless and non-invasive way. From a patient perspective, applying drugs on skin also provides stable dosage in blood so as to give the optimal bioavailability
In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation.
By definition, when a medication is administered intravenously, its bioavailability is 100%. H ...
and therapeutic effect
Therapeutic effect refers to the response(s) after a treatment of any kind, the results of which are judged to be useful or favorable. This is true whether the result was expected, unexpected, or even an unintended consequence. An adverse effect (i ...
s. In case of overdose
A drug overdose (overdose or OD) is the ingestion or application of a drug or other substance in quantities much greater than are recommended. or unwanted side effects, patients can take off or wash out the medicines quickly to eliminate toxicity
Toxicity is the degree to which a chemical substance or a particular mixture of substances can damage an organism. Toxicity can refer to the effect on a whole organism, such as an animal, bacterium, or plant, as well as the effect on a subst ...
by simply removing the patch to stop the delivery of drugs.
Disadvantages of topical drug delivery systems
The site of putting the patches for topical drugs may get irritated and have rash
A rash is a change of the human skin which affects its color, appearance, or texture.
A rash may be localized in one part of the body, or affect all the skin. Rashes may cause the skin to change color, itch, become warm, bumpy, chapped, dry, cr ...
es and feel itchy. Hence, some topical drugs including nicotine patch
A nicotine patch is a transdermal patch that releases nicotine into the body through the skin. It is used in nicotine replacement therapy (NRT), a process for smoking cessation. Endorsed and approved by the U.S. Food and Drug Administration (FDA) ...
es for smoking cessation
Smoking cessation, usually called quitting smoking or stopping smoking, is the process of discontinuing tobacco smoking. Tobacco smoke contains nicotine, which is addictive and can cause dependence. As a result, nicotine withdrawal often make ...
are advised to change places for each application to avoid continuous irritation of the skin. Also, since the drug needs to penetrate the skin, some drugs may not be able to pass through the skin. Some drugs are then “wasted” and the bioavailability of the drug will decrease.
Challenges for designing topical dosage form
Skin penetration is the main challenge for any topical dosage form. The drug needs to penetrate the skin in order to get into the body to apply its function. The drug follows the Fick’s first law of diffusion.[Florence, A. T., & Attwood, D. (2016). Physicochemical principles of
pharmacy in manufacture, formulation and clinical use. London:
(PhP) Pharmaceutical Press.] One of the most common versions of Fick’s first law of diffusion is:
:
where
* is the diffusion flux
Fick's laws of diffusion describe diffusion and were derived by Adolf Fick in 1855. They can be used to solve for the diffusion coefficient, . Fick's first law can be used to derive his second law which in turn is identical to the diffusion equ ...
.
* is the diffusion coefficient
Diffusivity, mass diffusivity or diffusion coefficient is a proportionality constant between the molar flux due to molecular diffusion and the gradient in the concentration of the species (or the driving force for diffusion). Diffusivity is enco ...
.
* is the concentration gradient
Molecular diffusion, often simply called diffusion, is the thermal motion of all (liquid or gas) particles at temperatures above absolute zero. The rate of this movement is a function of temperature, viscosity of the fluid and the size (mass) of ...
.
For is described by the Stokes–Einstein equation
In physics (specifically, the kinetic theory of gases), the Einstein relation is a previously unexpected connection revealed independently by William Sutherland in 1904, Albert Einstein in 1905, and by Marian Smoluchowski in 1906 in their works on ...
. The equation is:
:
where
* is the gas constant
The molar gas constant (also known as the gas constant, universal gas constant, or ideal gas constant) is denoted by the symbol or . It is the molar equivalent to the Boltzmann constant, expressed in units of energy per temperature increment per ...
.
* is the temperature
Temperature is a physical quantity that expresses quantitatively the perceptions of hotness and coldness. Temperature is measured with a thermometer.
Thermometers are calibrated in various temperature scales that historically have relied o ...
.
* is the viscosity
The viscosity of a fluid is a measure of its resistance to deformation at a given rate. For liquids, it corresponds to the informal concept of "thickness": for example, syrup has a higher viscosity than water.
Viscosity quantifies the inte ...
.
* is the radius
In classical geometry, a radius ( : radii) of a circle or sphere is any of the line segments from its center to its perimeter, and in more modern usage, it is also their length. The name comes from the latin ''radius'', meaning ray but also the ...
of the solute.
* is the Avogadro constant
The Avogadro constant, commonly denoted or , is the proportionality factor that relates the number of constituent particles (usually molecules, atoms or ions) in a sample with the amount of substance in that sample. It is an SI defining con ...
.
Assuming concentration gradient
Molecular diffusion, often simply called diffusion, is the thermal motion of all (liquid or gas) particles at temperatures above absolute zero. The rate of this movement is a function of temperature, viscosity of the fluid and the size (mass) of ...
is constant for all newly applied topical drugs and the temperature is constant (normal body temperature: 37 °C), the viscosity and radius of the drug determine the flux of diffusion. The higher the viscosity
The viscosity of a fluid is a measure of its resistance to deformation at a given rate. For liquids, it corresponds to the informal concept of "thickness": for example, syrup has a higher viscosity than water.
Viscosity quantifies the inte ...
or the larger the radius of the drug is, the lower the diffusion flux
Fick's laws of diffusion describe diffusion and were derived by Adolf Fick in 1855. They can be used to solve for the diffusion coefficient, . Fick's first law can be used to derive his second law which in turn is identical to the diffusion equ ...
of the drug is.
New developments
There are many factors for drug developers to consider in developing new topical formulations.
The first one is the effect of the vehicle
A vehicle (from la, vehiculum) is a machine that transports people or cargo. Vehicles include wagons, bicycles, motor vehicles (motorcycles, cars, trucks, buses, mobility scooters for disabled people), railed vehicles (trains, trams), wa ...
. The medium to carry the topical drugs can affect the penetration of the drug active ingredient
An active ingredient is any ingredient that provides biologically active or other direct effect in the diagnosis, cure, mitigation, treatment, or prevention of disease or to affect the structure or any function of the body of humans or animals. T ...
and efficacy
Efficacy is the ability to perform a task to a satisfactory or expected degree. The word comes from the same roots as ''effectiveness'', and it has often been used synonymously, although in pharmacology a pragmatic clinical trial#Efficacy versu ...
. For example, this carrier can have a cooling, drying, emollient or protective action to suit the required conditions of the application site such as applying gel
A gel is a semi-solid that can have properties ranging from soft and weak to hard and tough. Gels are defined as a substantially dilute cross-linked system, which exhibits no flow when in the steady-state, although the liquid phase may still di ...
or lotion
Lotion is a low-viscosity topical preparation intended for application to the skin. By contrast, creams and gels have higher viscosity, typically due to lower water content. Lotions are applied to external skin with bare hands, a brush, a clean ...
for hairy areas. Meanwhile, scientists need to match the type of preparation with the type of lesions. For example, they need to avoid oily ointments
A topical medication is a medication that is applied to a particular place on or in the body. Most often topical medication means application to body surfaces such as the skin or mucous membranes to treat ailments via a large range of classes ...
for acute weepy dermatitis
Dermatitis is inflammation of the skin, typically characterized by itchiness, redness and a rash. In cases of short duration, there may be small blisters, while in long-term cases the skin may become thickened. The area of skin involved can v ...
. Chemists also need to consider the irritation
Irritation, in biology and physiology, is a state of inflammation or painful reaction to allergy or cell-lining damage. A stimulus or agent which induces the state of irritation is an irritant. Irritants are typically thought of as chemical age ...
or any sensitization
Sensitization is a non-associative learning process in which repeated administration of a stimulus results in the progressive amplification of a response. Sensitization often is characterized by an enhancement of response to a whole class of stim ...
potential to ensure that the topical application can be stable during storage and transport to maintain its efficacy. Another potential material is nanofiber-based dispersion to improve the adhesion of active ingredients on the skin.
In order to enhance drug penetration into the skin, scientists have several ways to achieve their purposes by using chemical, biochemical, physical and super saturation
In physical chemistry, supersaturation occurs with a solution (chemistry), solution when the concentration of a solute exceeds the concentration specified by the value of solubility at Solubility equilibrium, equilibrium. Most commonly the term ...
enhancement. Advanced Emulgel technology is a breakthrough of painkilling topical drugs. It helps the gel to enter deeply down the skin layer to strengthen delivery of diclofenac to the point of pain so as to achieve better therapeutic effect
Therapeutic effect refers to the response(s) after a treatment of any kind, the results of which are judged to be useful or favorable. This is true whether the result was expected, unexpected, or even an unintended consequence. An adverse effect (i ...
s by modifying the above properties.
See also
* Finger tip unit In medicine, a finger tip unit (FTU) is defined as the amount of ointment, cream or other semi-solid dosage form expressed from a tube with a 5 mm diameter nozzle, applied from the distal skin-crease to the tip of the index finger of an adult.F ...
* Liniment
Liniment (from la, linere, meaning "to anoint"), also called embrocation and heat rub, is a medicated topical preparation for application to the skin. Some liniments have viscosity similar to that of water; others are lotion or balm; still other ...
* Topical anesthetic A topical anesthetic is a local anesthetic that is used to numb the surface of a body part. They can be used to numb any area of the skin as well as the front of the eyeball, the inside of the nose, ear or throat, the anus and the genital area. Top ...
* Topical antibiotic
An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting bacterial infections, and antibiotic medications are widely used in the treatment and prevention of ...
* Topical corticosteroids Topical steroids are the topical forms of corticosteroids. Topical steroids are the most commonly prescribed topical medications for the treatment of rash, eczema, and dermatitis. Topical steroids have anti-inflammatory properties and are classifie ...
* Unguent
An unguent is a soothing preparation spread on wounds, burns, rashes, abrasions or other topical injuries (i.e. damage to the skin). It is similar to an ointment, though typically an unguent is oilier and less viscous. It is usually delivered as a ...
References
* Goodman & Gilman's The Pharmacological Basis of Therapeutics
''Goodman & Gilman's The Pharmacological Basis of Therapeutics'', commonly referred to as the Blue Bible or Goodman & Gilman, is a textbook of pharmacology originally authored by Louis S. Goodman and Alfred Gilman. First published in 1941, the b ...
* Dr. David Edwards - Dentistry Microbiology Lecture series
External links
History of ointments
{{Authority control
Medical terminology
Routes of administration
Ointments
Drug delivery devices
Dosage forms