A New Approach to Ex Vivo Permeation Studies in In-Situ Film-Forming Systems
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Research Article A New Approach to Ex Vivo Permeation Studies in In-Situ Film-Forming Systems Amanda F. Silva-Alvarez,1,3 Maíra P. Ferreira,1 Fabiana T. M. C. Vicentini,1 Vinicius Pedrazzi,2 and Osvaldo de Freitas1
Received 6 June 2020; accepted 18 August 2020 Abstract. The skin is the largest human organ and an important topical route. Even with some challenges, it is an important ally in medication administration, mainly because it is painless and easy-to-apply. Semisolid formulations are the most used dosage forms for drug administration via this delivery route and can be optimized when transformed into a film, favoring on-site maintenance, and promoting drug permeation. However, in situ film-forming systems are difficult to assess and characterize using Franz-type diffusion cells once this apparatus is ideal to formulations without transition phases. The present study proposed a different method to characterize these formulations and provide complementary data on drug and penetration enhancer behaviors, as close as possible to real application conditions. This characterization method allowed us to analyze drug concentration on three necessary occasions: remaining in the polymer film, stratum corneum using adhesive tape, and skin to check where drugs will have a desirable effect. As a proof-of-concept, the proposed ex vivo permeation method was used to evaluate a film-forming system containing lidocaine and prilocaine. We could also evaluate transition phases of drug compositions and quantify drugs at key times after application. Hence, the developed method may be used to provide complementary data to the Franz diffusion cell method, in terms of drug and penetration enhancer behaviors incorporated into film-forming delivery systems. KEY WORDS: film-forming composition; Franz diffusion cell; a permeation enhancer; permeability; epithelial drug delivery.
INTRODUCTION The skin is the first and main barrier against the entry of substances into the body. Besides offering protection against solar radiation and dehydration, the skin has an important function in homeostasis regulation. It is composed of three layers: epidermis, dermis, and hypodermis (1,2). On the outer surface of the epidermis, there is another layer of dead and keratinized cells dispersed in a lipid matrix, denominated stratum corneum (SC). This organized structure is responsible for drug low permeability and hindered transport across the skin (2).
Electronic supplementary material The online version of this article (https://doi.org/10.1208/s12249-020-01799-6) contains supplementary material, which is available to authorized users. 1
Laboratório de P&D Farmacotécnico, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo (USP), Ribeirão Preto, SP, Brazil. 2 Faculdade de Odontologia de Ribeirão Preto, Universidade de São Paulo (USP), Ribeirão Preto, SP, Brazil. 3 To whom correspondence should be addressed. (e–mail: [email protected])
Despite some challenges, the topical route is an important mode of drug administration, mainly
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