Topical formulations

General principals
Topical formulations are applied directly to the skin. Advantages of this include:

Increased dose of medication where it is needed Reduced side effects and toxicity to other organs

Disadvantages include:

Time consuming At times, complicated e.g. if several different formulations have been prescribed May be messy or uncomfortable

Topical formulations are made up in a vehicle, or base, which may be optimised for a particular site of the body or type of skin condition. The product may be designed to be moisturising or to maximise the penetration of an active ingredient, a medicine, into or through the skin. The amount of the active ingredient that is absorbed through the skin depends on the following factors:

Skin thickness this varies with body site, age, skin disorder: thin skin absorbs more. Skin barrier function horny cell layer disrupted by dermatitis, ichthyosis and keratolytic agents such as salicylic acid and absorbs more. Skin hydration up to 10 times more absorption if occluded e.g. skin folds or under a dressing or greasy ointment. Molecular size of the chemical: small molecules are more easily absorbed. Whether the chemical is lipophilic lipophilic agents are better absorbed through the horny cell layer which is made up of lipids including ceramides, cholesterol and fatty acids. Chemical concentration stronger concentrations may penetrate more effectively. Other ingredients in the formulation may interact to increase or reduce potency or absorption rates.

For these reasons, although generic formulations may apparently contain the same active ingredient and at the same concentration as the brand original, the effectiveness may be different.

Quantity
Normally, topical medications should be applied to the skin as a thin layer. Expect 1 gram of cream to spread out over a 10cm2 area of skin and an ointment spreads a little further. The fingertip unit (0.5g) is a guide to the amount of a cream or ointment needed to treat an area for a certain time. One fingertip unit covers one side of 2 flat hands and one gram covers both sides of the two hands. It takes 20 to 30g of cream or ointment to cover an adult once.

Vehicles
Topical formulations contain an active ingredient, often a medication or drug or botanical, and a vehicle. The vehicle contains water, oil, alcohol or propylene glycol mixed with preservatives, emulsifiers, absorption promoters and fragrances. The table below describes different formulations. Manufacturers interpret the definitions in various ways so a similar preparation might be called lotion, gel or cream.

Classification of topical formulations

Solution

Lotion

Usually considered thicker than a solution and more likely to contain oil as well as water or alcohol. A shake lotion separates into parts with time so needs to be shaken into suspension before use.

Cream

Thicker than a lotion, maintaining its shape, e.g., 50/50 emulsion of oil and water. Requires preservative to extend shelf life. Often moisturising.

Ointment

Semi-solid, water-free or nearly water-free (80% oil). Greasy, sticky, emollient, protective, occlusive. No need for preservative so contact allergy is rare. May include hydrocarbon (paraffin), wool fat, beeswax, macrogols, emulsifying wax, cetrimide or vegetable oil (olive oil, arachis oil, coconut oil). Aqueous or alcoholic monophasic semisolid emulsion, often based on cellulose and liquifies upon contact with skin. Often includes preservatives and fragrances.

Gel

Paste

Concentrated suspension of oil, water and powder

Aerosol foam or

Solution with pressurised propellant

spray

Powder

Solid e.g. talc (a mineral) or corn starch (vegetable)

Solid

EG antiperspirant stick. May melt on reaching body temperature e.g. suppositories.

Transdermal

Drug delivery system allows precise dosing: includes an adhesive.

patch

Other terms used by cosmetic and pharmaceutical manufacturers include emulsion, paint, suspension, milk, syrup, collodion, balm and mist. Formulae may have mixed ingredients with more than one type of vehicle. Factors in the choice of vehicle or base for a topical medication include the nature of the dermatosis and its site. When your pharmacist makes up a mixture, it is extemporaneously compounded. Galenicals is the name given to the crude ingredients (often natural in origin) they may be added to a vehicle or to a brand-name product.

Nature of the dermatosis

Site

Palms and soles: ointment or cream Skin folds: cream or lotion Hairy areas: lotion, solution, gel, foam

Mucosal surfaces: non-irritating formulations

Special circumstances
Newborn babies
The skin barrier of full term newborn babies is nearly the same as in older children and adults. However, the barrier function in premature babies is markedly impaired. The surface area of a baby is proportionally much greater than that of an adult. Organs such as liver, kidneys, blood and central nervous system are not fully developed. This means topically applied medications can be more likley to result in side effects and toxicity.

Pregnancy and lactation

Podophyllin Dithranol 5-Fluorouracil

Salicylic acid Medications are classified according to their risk. The FDA classification system is often used.
Pregnancy categories used in New Zealand

Category A

Drugs which have been taken by a large number of pregnant women and women of childbearing age without any proven increase in the frequency of malfor indirect harmful effects on the fetus having been observed.

Category B1

Drugs that have been taken by only a limited number of pregnant women and women of childbearing age, without an increase in the frequency of malforma

indirect harmful effects on the human fetus having been observed. Studies in animals[1] have not shown evidence of an increased occurrence of fetal dama

Category B2

Drugs that have been taken by only a limited number of pregnant women and women of childbearing age, without an increase in the frequency of malforma

indirect harmful effects on the human fetus having been observed. Studies in animals[1] are inadequate or may be lacking, but available data show no evid occurrence of fetal damage.

Category B3

Drugs that have been taken by only a limited number of pregnant women and women of childbearing age, without an increase in the frequency of malforma indirect harmful effects on the human fetus having been observed. Studies in animals[1] have shown evidence of an increased occurrence of fetal damage, considered uncertain in humans.

Category C

Drugs that, owing to their pharmacological effects, have caused or maybe suspected of causing harmful effects on the human fetus or neonate without caus effects may be reversible.

Category D

Drugs that have caused, are suspected to have caused or may be expected to cause an increased incidence of human fetal malformations or irreversible da have adverse pharmacological effects.

Category X

Drugs that have such a high risk of causing permanent damage to the fetus that they should not be used in pregnancy or when there is a possibility of preg

Tips for using topical agents

Topical steroids and emollients are more effective if the skin is slightly wet. So the most effective time to apply them is within 3 minutes after a bath or shower. Apply the steroid to active areas only. If you are also prescribed emollient, wait a few minutes for the topical steroid to penetrate, then apply emollient widely.

Complaints that products sting on facial skin are common, especially if the skin is damp at the time of application. Wait 20 minutes and the stinging is often much less troublesome. Stinging is common with lotions and creams and sometimes also occurs with ointments. A change of formulation rather than medicament may solve the problem. Sometimes it is best to put up with stinging, which often only lasts a few minutes, because after a few applications of an effective treatment the skin heals and stinging lessens.

If it is difficult to squeeze out a cream or ointment, cut off the end of tube. Note that this may invalidate the expiry date and increase the chance of contamination of the product.