Preparation of Neogambogic Acid Nanoliposomes and its Pharmacokinetics in Rats.

ABSTRACT

OBJECTIVE: To prepare neogambogic acid nanoliposomes (GNA-NLC) and study its pharmacokinetics (PK) in rats. STUDY DESIGN: An experimental study. PLACE AND DURATION OF STUDY Mudanjiang Medical University, Mudanjiang, China, from January 2016 to October 2017. METHODOLOGY: GNA-NLC was prepared by emulsion evaporation-low temperature solidification. The entrapment efficiency, average particle size, and zeta potential were investigated. Male Wistar rats were injected with 1 mg/mL gambogic acid and GNA-NLC into the caudal vein respectively, and the plasma concentration was determined by UPLC- MS/MS. The pharmacokinetic parameters of the two agents were compared. RESULTS: GNA-NLC prepared in this study were mostly spherical spheroids with an average particle size of 146.35 ±1.72 nm, polydispersity coefficient of 0.26 ±0.02, zeta potential of -28.24 ±0.13 MV, entrapment efficiency of 84.63%, and drug loading capacity of 4.23%. DSC showed that neogambogic acid nanoparticles had formed and neogambogic acid was amorphous in the matrix. The pharmacokinetics results in rats showed that GNA-NLC plasma concentration was significantly higher than that of common preparation of gambogic acid, with a half-life period of 10.14 ±0.03 hours, 4.57 times that of gambogic acid. AUC0 ~ 24h of gambogic acid in GNA-NLC lipidosome was 58.36 ±0.23 μg/h/mL, 4.83 times that of gambogic acid. CONCLUSION: GNA-NLC can be prepared successfully by emulsion evaporation-low temperature solidification. The method is simple and easy to control. The GNA-NLC has a long cycle, and high blood concentration, sustained release compared with the raw material gambogic acid.