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An Overview of Pharmaceutical Topical Formulation Development
Topical formulations are a vital part of pharmaceutical development. As it’s
applied directly to the skin, most of the patients prefer this dosage form.
Advantages of topical formulations
An increased dose of medication is applied where it is needed.
There are reduced side effects and toxicity to other organs compared to
systemic medications.
Disadvantages of topical formulations
They can be time consuming to apply.
Sometimes, the regimen can be complicated, especially if several different
formulations have been prescribed.
The applications may also 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,
often a medicine, into or through the skin.
Topical formulation absorption / penetration through the skin depends on the
following factors:
Thin skin absorbs more than thick skin — skin thickness varies with body
site, age and the specific skin disorder
Skin barrier function — this may be disrupted by dermatitis, ichthyosis and
keratolytic agents (such as salicylic acid), so it may absorb more medication
than intact, normal skin
The absorption of the active ingredient is greater where there is occlusion,
such as in the skin folds, under dressings, or when a greasy, ointment
formulation is used
Small molecules are more easily absorbed through the skin than large
molecules
Lipophilic compounds are better absorbed than hydrophilic compounds
Higher concentrations of the active ingredient may penetrate more than
lower concentrations
Other ingredients in the formulation may interact to increase or reduce
potency or absorption rates.
Note: Minor differences in formulation may make surprising differences to the
effectiveness of a topical medication.
Topical Formulation Excipients
Structure forming agents
Cetosteryl alcohol, Sorbitan, Mineral oils etc.
Preservatives
Benzyl alcohol, Sodium benzoate, Methyl paraben, Propyl paraben,
Chlorocresol etc.
Antioxidants
Butyl hydroxyl toluene, Butyl hydroxyl anisole, Ascorbic acid etc.
Solubilizers
Lanolin, Cholesterol, Cholesterol esters etc.
Gelling agents
Carbomer, Carboxy methyl cellulose, Hydroxyl propyl cellulose, Xanthan
gum etc.
Emollients
Glycerin, Mineral oil, Petrolatum, Isopropyl palmitate etc.
Suppository bases
Cocoa butter, Glycerin, Coconut oil, Gelatin, Hydrogenated vegetable oil,
Polyethylene glycol etc.
Dermal Topical Formulation Types
Cream formulation: Thicker than a lotion, maintaining its shape, for
example a 50/50 emulsion of oil and water. Requires preservative to extend
shelf life. Often moisturizing.
Ointment formulation: 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).
Solution formulation: Water or alcoholic lotion containing a dissolved
powder.
Lotion formulation: 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.
Gel formulation: Aqueous or alcoholic monophasic semisolid emulsion,
often based on cellulose and liquefies upon contact with skin. Often includes
preservatives and fragrances.
Paste formulation: Concentrated suspension of oil, water and powder.
Spray formulation:
Aerosol foam or spray: Solution with pressurized propellant.
Powder formulation: Powder Solid, for example talc (a mineral) or corn
starch (vegetable). Powder formulation
Solid formulation: Antiperspirant or sunscreen stick. May melt on
reaching body temperature (eg, a suppository).
Patch formulation: Drug delivery system allows precise dosing: includes
an adhesive.
The site of topical formulation
Palms and soles — an ointment or cream may be preferred.
Skin folds — use a cream or a lotion (ointments are too occlusive for these
sites)
Hairy areas — a lotion, solution, gel, or foam is usually best.
Mucosal surfaces — take care to prescribe non-irritating formulations to
avoid irritating eroded surfaces.
pH of topical formulation
The pH of topical formulation commonly suggest to adjust with skin. From this
aspect the pH range fall between 5 to 7. But depending on the stability of topical
formulation the pH range can slightly vary.
Storage of topical formulation
Topical formulation should be stored in the indicated storage condition. Otherwise
the efficacy of the formulation can be reduced or declined due through phase
separation or denature of the product.
Reference: Pharma guideline, brainkart, pharma specialists
