%0 Journal Article
%T Sodium Alginate/Chitosan-Coated Liposomes for Oral Delivery of Hydroxy-α-Sanshool: In Vitro and In Vivo Evaluation.
%A Tan F
%A Li H
%A Zhang K
%A Xu L
%A Zhang D
%A Han Y
%A Han J
%J Pharmaceutics
%V 15
%N 7
%D 2023 Jul 24
%M 37514196
%F 6.525
%R 10.3390/pharmaceutics15072010
%X BACKGROUND: Hydroxy-α-Sanshool (HAS) possesses various pharmacological properties, such as analgesia and regulating gastrointestinal function. However, the low oral bioavailability of HAS has limited its oral delivery in clinical application.
RESULTS: To enhance its oral bioavailability, a nanocomposite delivery system based on chitosan (CH, as the polycation) and sodium alginate (SA, as the polyanion) was prepared using a layer-by-layer coating technique. The morphology, thermal behavior and Fourier transform infrared spectrum (FTIR) showed that the obtained sodium alginate/chitosan-coated HAS-loaded liposomes (SA/CH-HAS-LIP) with core-shell structures have been successfully covered with polymers. When compared with HAS-loaded liposomes (HAS-LIP), SA/CH-HAS-LIP displayed obvious pH sensitivity and a sustained-release behavior in in vitro studies, which fitted well to Weibull model. In vivo, the half-life of HAS from SA/CH-HAS-LIP remarkably extended after oral administration compared to the free drug. Additionally, it allowed a 4.6-fold and 4.2-fold increase in oral bioavailability, respectively, compared with free HAS and HAS-LIP.
CONCLUSIONS: SA/CH-HAS-LIP could be a promising release vehicle for the oral delivery of HAS to increase its oral bioavailability.