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To prepare polyethylene glycol succinate-vitamin E modified pinocembrin (PCB)-loaded liposomes (PCBT-liposomes) and evaluate PCBT-liposomal pharmacokinetics and antihyperglycemic activity. The novel PCBT-liposomes demonstrated a promising application prospect as a nano drug carrier for future research. 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. 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 °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  Cmax , MRT 0–t, and  T1/2  of PCBT-liposomes were roughly 1.700 ± 0.139 µg·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-α (TNF-α) concentrations in serum of diabetic mice were respectively decreased 28.28%, 17.23%, 17.77%, and 8.08% after PCBT-liposomal treatment. 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.

drug development and industrial pharmacy

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