Preparation, in vitro and in vivo evaluation of pinocembrin-loaded TPGS modified liposomes with enhanced bioavailability and antihyperglycemic activity

Purpose To prepare polyethylene glycol succinate-vitamin E modified pinocembrin (PCB)-loaded liposomes (PCBT-liposomes) and evaluate PCBT-liposomal pharmacokinetics and antihyperglycemic activity. Significance The novel PCBT-liposomes demonstrated a promising application prospect as a nano drug carrier for future research. Methods Thin film dispersion was used to prepare PCBT-liposomes. We measured a series of characterization, followed by in vitro cumulative release, in vivo pharmacokinetic study, and antihyperglycemic activity evaluation. Results PCBT-liposomes displayed spherical and bilayered nanoparticles with mean particle size (roughly 92 nm), negative zeta potential (about -26.650 mV), high drug encapsulation efficiency (87.32 +/- 1.34%) and good storage (at 4 or 25 degrees C) stability during 48 h after hydration. The cumulative release rate of PCBT-liposomes was markedly higher than free PCB in four different pH media. In vivo investigation showed that PCBT-liposomes could obviously improve oral bioavailability of PCB by 1.96 times, whereas the C (max), MRT0- (t) , and T (1/2) of PCBT-liposomes were roughly 1.700 +/- 0.139 mu g center dot mL(-1), 12.695 +/- 1.647 h, and 14.244 h, respectively. In terms of biochemical analysis, aspartate amino-transferase (AST), alanine amino-transferase (ALT), interleukin-1 (IL-1), and tumor necrosis factor-alpha (TNF-alpha) concentrations in serum of diabetic mice were respectively decreased 28.28%, 17.23%, 17.77%, and 8.08% after PCBT-liposomal treatment. Conclusion These results show PCBT-liposomal preparation as an excellent nano-carrier which has the potential to improve water solubility, bioavailability, and antihyperglycemic activity of PCB, amid broadening the application of PCB in the clinical settings.

Automated summary

This study successfully prepared polyethylene glycol succinate-vitamin E modified pinocembrin-loaded liposomes and evaluated their pharmacokinetics and antihyperglycemic activity. The PCBT-liposomes showed promising potential as a nano drug carrier and demonstrated improved water solubility, bioavailability, and antihyperglycemic activity of PCB.