Comparison of Caffeine (CAF) Penetration Using PLGA Nanoparticle and Aqueous Formulations: An In Vitro Study with Franz Diffusion Cell

Abstract

Caffeine (CAF) is a non-selective adenosine A1 receptor antagonist which predominates in fat cells. When CAF binds to adenosine receptors, it increases cyclic adenosine monophosphate; inhibiting adipogenesis and inducing fat lipolysis. This study aimed to evaluate using the method of Franz diffusion cells, the caffeine (CAF) releasing profiles of two forms: A nanoparticle PLGA and a pure water for injection. Drug release analysis was carried out under physiological conditions (pH: 5.6 to 7.4; ionic strength 0.15 M; at 25 °C) for 8 h. One independent vertical Franz cells were used with a nominal volume of the acceptor compartment of 12.0 mL and a diffusion area of 1.77 cm2.  A transdermal simulation type (Strat-M®) type membranes is used. The CAF permeation profiles demonstrated on the membrane type and the vehicle used, the permeation is strongly affected. High permeation efficiencies were obtained for the CAF nanoparticle form, and low effect was observed for CAF water for injection formulation. The permeation studies membranes represent a reproducible method, which is easy to implement for pre-formulation stage or performance evaluation of pharmaceutical products for topical purposed administration.