Preparation of Prolonged-Circulating Galangin-Loaded Liposomes and Evaluation of Antitumor Efficacy In Vitro and Pharmacokinetics In Vivo

Abstract

Galangin has been reported to have many pharmacological effects including being anti-inflammatory, antibacterial, and antifungal and a suppressor of vitiligo, Alzheimer’s disease, and cancer. The purpose of this research was to characterize and determine the efficacy of the antitumor activity and pharmacokinetics of galangin-loaded PEGylated liposomes compared with free galangin. Galangin-loaded liposomes and galangin-loaded PEGylated liposomes were prepared using thin-film dispersion prior to ultrasonication. The mean particle size of the galangin-loaded PEGylated liposomes was approximately 120 nm, the polydispersity index was 0.212, the zeta potential was -2.24 mV, and the entrapment efficiency was 76.31%. The release of galangin from galangin-loaded PEG-modified liposomes was slowest as gauged by dynamic dialysis in vitro. In the apoptosis experiment, galangin-loaded PEG-modified liposomes demonstrated cytotoxicity to hepatoma cells by apoptosis that was greater than the two other forms of drug carrier. In vivo experiments demonstrated that the half-life of galangin in PEG-modified liposomes was 4 hours in the plasma of rats, significantly longer than that of free galangin. The experimental results suggest that the PEG modification of liposomes effectively increases the solubility of galangin and alters its pharmacokinetic parameters, such that it may be effective in the treatment of liver cancer.