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Rapid Pharmacokinetic Evaluation of Topical Drug Formulations

Author(s):  Garzouzi Victoria L, Reifenrath William G

Issue:  Jul/Aug 1999 - Compounding Parenteral Products
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Abstract:  A new in vitro test system was developed to efficiently determine the effect of formulation on topical drug delivery.

Sheets of viable, excised pig skin were sandwiched between two standard 24-well plates. The lower wells contained receptor fluid and a magnetic stirrer. The upper wells were opened to the atmosphere for formulation application. Using 14Csalicylic acid as a model compound, eight different formulations were evaluated representing hydrophilic and lipophilic solutions, a suspension and o/w and w/o emulsions. Formulations were applied to the skin surface in six different wells on three sets of plates. Twenty-four hours after application, excess drug was wiped from the skin surface and assayed for radiolabel. The stratum corneum was removed by tape stripping and radiolabel determined by electronic autoradiography. Radiolabel contained in the remaining epidermis, dermis and receptor fluid was also determined.

Statistical analysis (ANOVA, Student-Newman-Keuls multiple- range test, p=0.05) of radiolabel penetrating into the dermis and receptor fluid revealed the following order of formulations: ethanol = aqueous surfactant < o/w emulsion = w/o emulsion

Related Keywords: skin, suspensions, topical drug delivery


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