In vitro release of selected nonsteroidal antiinflammatory analgesics [NSAIA] from reservoir-type transdermal formulations

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Abstract
Indomethacin [I], Ketoprofen [II] and Sulindac [III] were evaluated for in vitro percutaneous uptake from various ointment bases. Three doses for each NSAIA were employed for evaluation. Each reservoir system was evaluated for drug release across composite skin (semipermeable membrane) using a modified FDC assembly over a 12 h period. The drug release profiles were examined for mechanism of drug release and developing recommendations for designing a dermal product for a NSAIA. For all NSAIAs: This study demonstrated that I, II and III can penetrate the composite skin barrier with differing efficiencies. II penetrated with maximal ease while I with minimal ease. The drug release rate increased with increasing drug load. 0/W and water soluble system compositions yielded superior drug release rates when compared to other reservoir systems. The drug release characteristics indicated adherence to diffusional pathways borne out of Q versus square-root-of-time relationship. The Qmax:Drug Load (Dose) ratio as a function of Dose was influenced by the compositional characteristics for any given system. Statistically significant differences (p<0.01) were observed when apparent permeability coefficients were compared between various compositions and within the dose levels for each composition tested.

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