Abstract:

This study aimed to investigate the pharmacokinetic properties of ginkgetin TPGS/Soluplus mixed nano-micelles (ginkgetin nanomicelles) in rats. The nanomicelles were prepared using the film hydration method and subsequently characterized in terms of particle size, zeta potential, drug loading, entrapment efficiency, and critical micelle concentration. The oral pharmacokinetic profile of the nanomicelles was compared with that of free ginkgetin. Sprague-Dawley rats were randomly assigned to either the ginkgetin group or the ginkgetin nanomicelles group, with six rats per group. Each group received an intragastric dose of 100 mg/kg (calculated based on the ginkgetin content). Blood samples were collected from the inner canthus at designated time points, and pharmacokinetic parameters were calculated. The prepared ginkgetin nanomicelles exhibited an average particle size of 66.33 ± 2.11 nm, a polydispersity index of 0.061 ± 0.013, and a zeta potential of –25.67 ± 0.21 mV. The entrapment efficiency and drug loading were 97.92% ± 0.66% and 2.47% ± 0.02%, respectively. Pharmacokinetic analysis revealed that, compared with free ginkgetin, the nanomicelles significantly prolonged t_max and t_1/2, and increased C_max, AUC_0–t, and AUC_0–∞ (P < 0.05). The analytical method established in this study proved effective for determining ginkgetin concentrations. Oral administration of ginkgetin nanomicelles markedly enhanced the bioavailability of ginkgetin.

Key words: Ginkgetin, TPGS/Soluplus, Nano-micelles, Pharmacokinetics, Bioavailability