CAPSAICIN-VITAMIN E PRODRUG SELF-ASSEMBLED NANOPARTICLE, AND PREPARATION METHOD THEREFOR AND USE THEREOF

摘要

Disclosed is the preparation of a capsaicin-vitamin E prodrug self-assembled nano drug delivery system, which uses dithiodiglycolic acid to link capsaicin to vitamin E to prepare a capsaicin-vitamin E prodrug (Cap-SVE). On this basis, capsaicin-vitamin E prodrug self-assembled nanoparticles (Cap-SVE NPs) are further prepared. The prodrug self-assembled nanoparticles have some characteristics: the average particle size of less than 200 nm, being near-spherical and uniformly distributed, and the drug loading capacity calculated with capsaicin of up to 8 mg·mL-1. It is stable under acidic conditions and gradually hydrolyzes at pH 7.4. The prodrug self-assembled nanoparticles can reduce the irritation of capsaicin on the gastrointestinal tract, significantly increase the bioavailability of capsaicin, increase the targeting effect of capsaicin in the liver, and significantly improve the anti-oxidative and hypolipidemic efficacy of capsaicin. It has good stability, high safety, and a large market prospect.