In Vitro Efficacy and Release Study with Anti-Inflammatory Drugs Incorporated in Adhesive Transdermal Drug Delivery Systems

Abstract

<h2>ABSTRACT</h2> The topical application of two different anti-inflammatory extracts incorporated in adhesive transdermal drug delivery systems (TDDSs) was investigated. Therefore, anti-inflammatory properties and percutaneous absorption behavior of adhesive TDDSs were characterized <i>in vitro</i> conducting experiments with a dermatologically relevant human skin model. Anti-inflammatory efficacy against UV irradiation of both TDDSs was determined <i>in vitro</i> with EpiDerm™. The reduction of the release of proinflammatory cytokines by topically applied TDDSs was compared with the reduction during the presence of the specific cyclooxygenase inhibitor diclofenac in the culture medium. A similar anti-inflammatory efficacy of the topically applied TDDSs in comparison with the use of diclofenac in the culture medium should be achieved. Furthermore, percutaneous absorption in efficacy tests was compared with percutaneous absorption in diffusion studies with porcine cadaver skin. Both the topically applied TDDSs showed a significant anti-inflammatory activity. Permeation coefficients through the stratum corneum and the epidermis gained from the release studies on porcine cadaver skin (<i>Magnolia</i>: 2.23·10⁻⁵ cm/h, licorice: 4.68·10⁻⁶ cm/h) were approximately five times lower than the permeation coefficients obtained with the EpiDerm™ skin model (<i>Magnolia</i>: 9.48·10⁻⁵ cm/h, licorice: 24.0·10⁻⁶ cm/h). Therefore, an adjustment of drug doses during experiments with the EpiDerm™ skin model because of weaker skin barrier properties should be considered. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:1142–1148, 2014