摘要：

The aim of this study was to assess the rate and extent of transcutaneous delivery of prostaglandin E 1 (PGE 1 ) from various formulations [liposomal, novel biphasic, and nonliposomal (oil/water cream) delivery systems] in vitro using diffusion cells and in vivo using laser doppler flowmetry, to aid in the development of a topically active preparation for the treatment of male sexual dysfunction. Percutaneous absorption through adult human foreskin was tested in flow-through diffusion cells using [ 3 H]PGE 1> . Nine healthy volunteers participated in the crossover, randomized, double-blind, placebo-controlled study, where 0.1 g of each preparation was applied to a 4 cm 2 area on the forearm. Laserflo BPM 2 blood perfusion monitor with Model P-430 skin probe was used for evaluating skin blood perfusion. Encapsulation of PGE 1 into novel biphasic delivery systems resulted in significantly increased skin blood perfusion relative to traditional liposomal, nonliposomal, and placebo formulations (6.25 ± 1.58 vs 2.72 ± 0.79, 0.53 ± 0.64, and 0.58 ± 0.06 mL LD /min/100 g, respectively, n = 9). The in vitro absorption of PGE 1 through foreskin correlated well with the in vivo data (respective permeability coefficients 3.33, 1.57, and 1.40 ± 10 4 cm/h). Formulation parameters greatly influence the absorption of PGE 1 through skin as measured by laser doppler flowmetry, but by the application of a novel topical delivery technology, a significant enhancement of PGE 1 delivery can be achieved.

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