Resumo

SERRANO CASTANEDA, Pablo et al. Microneedles and Transcutol® as transdermal penetration enhancers of sibutramine formulated in a transdermal patch. Rev Cubana Farm [online]. 2013, vol.47, n.3, pp. 289-299. ISSN 0034-7515.

Introduction: the main permeation barrier is the skin. Although it is almost an impermeable barrier to most substances, new ways have been examined to improve its permeability by using new technologies such as microneedles and chemical enhancers like Transcutol^®. Objective: to develop and to characterize a transdermal patch containing sibutramine hydrochloride as model drug and using microneedles and Transcutol^® as transdermal drug delivery enhancers. Methods: Physicochemical characterization of sibutramine hydrochloride patches using polarized light microscopy, bioadhesion, tensile strength studies. The diffusion studies were performed in Franz-type diffusion cells with human abdominal skin as a sort of membrane between both compartments. The active ingredient was quantified through capillary electrophoresis. Results: bioadhesive patches were obtained, with adequate stability of sibutramine hydrochloride in the polymer matrix of chitosan. The use of microneedles and Transcutol^® increased sibutramine hydrochloride delivery through the human skin when compared with the control patch. The flow rates were 0.0649 mg.cm^-2.h^-1 and 0,0816 mg.cm^-2.h^-1 in the enhanced patch by using 1 and 2 mm microneedles respectively, in comparison with flow rates of 0,0527 mg.cm^-2.h^-1 and 0.0554 mg.cm^-2.h^-1 for the control patch having no enhancing agent with 1 and 2 mm microneedles respectively. Conclusions: the results show that it is possible to use Transcutol^® and microneedles to increase the delivery of potent drugs having a structure similar to that of sibutramine through transdermal administration. All this generates new alternatives to oral pharmaceuticals in order to treat ailments and diseases.

Palavras-chave : microneedles; Transcutol; physical and chemical enhancers; transdermal patch; skin.

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