Garcinol loaded vitamin E TPGS emulsified PLGA nanoparticles: preparation, physicochemical characterization, in vitro and in vivo studies

摘要

Garcinol (GAR) is a naturally occurring polyisoprenylated phenolic compound. It has been recentlyudinvestigated for its biological activities such as antioxidant, anti-inflammatory, anti ulcer, andudantiproliferative effect on a wide range of human cancer cell lines. Though the outcomes are veryudpromising, its extreme insolubility in water remains the main obstacle for its clinical application. Hereinudwe report the formulation of GAR entrapped PLGA nanoparticles by nanoprecipitation method usingudvitamin E TPGS as an emulsifier. The nanoparticles were characterized for size, surface morphology,udsurface charge, encapsulation efficiency and in vitro drug release kinetics. The MTT assay depicted audhigh amount of cytotoxicity of GAR-NPs in B16F10, HepG2 and KB cells. A considerable amount of celludapoptosis was observed in B16f10 and KB cell lines. In vivo cellular uptake of fluorescent NPs on B16F10udcells was also investigated. Finally the GAR loaded NPs were radiolabeled with technetium-99m withud>95% labeling efficiency and administered to B16F10 melanoma tumor bearing mice to investigate theudin vivo deposition at the tumor site by biodistribution and scintigraphic imaging study. In vitro cellularuduptake studies and biological evaluation confirm the efficacy of the formulation for cancer treatment