College of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, China.
College of Chinese Medicine, Hunan University of Chinese Medicine, Changsha, 410208, China.
Sci Rep. 2023 Oct 27;13(1):18472. doi: 10.1038/s41598-023-45858-x.
This study aimed to construct a Ginsenoside Rb1-PLGA nano drug delivery system, optimize its preparation process, characterize and evaluate the resulting Ginsenoside Rb1-PLGA Nanoparticles (GRb1@PLGA@NPs). GRb1@PLGA@NPs were prepared using the emulsion solvent evaporation method. The optimal preparation process was determined using Plackett-Burman design combined with Box-Behnken experiments. Physical characterization and in vitro release studies were conducted. LC-MS/MS technique was employed to investigate the pharmacokinetic characteristics of GRb1 and GRb1@PLGA@NPs in rat plasma. The optimal preparation process yielded GRb1@PLGA@NPs with a particle size of 120.63 nm, polydispersity index (PDI) of 0.172, zeta potential of - 22.67 mV, encapsulation efficiency of 75%, and drug loading of 11%. In vitro release demonstrated sustained drug release. Compared to GRb1, GRb1@PLGA@NPs exhibited a shortened time to peak concentration by approximately 0.72-fold. The area under the plasma concentration-time curve significantly increased to 4.58-fold of GRb1. GRb1@PLGA@NPs formulated using the optimal process exhibited uniform distribution and stable quality, its relative oral bioavailability was significantly improved compared to free GRb1.
本研究旨在构建人参皂苷 Rb1-PLGA 纳米药物传递系统,优化其制备工艺,对所得的人参皂苷 Rb1-PLGA 纳米粒(GRb1@PLGA@NPs)进行表征和评价。GRb1@PLGA@NPs 采用乳化溶剂蒸发法制备。采用 Plackett-Burman 设计结合 Box-Behnken 实验确定最佳制备工艺。进行物理特性表征和体外释放研究。采用 LC-MS/MS 技术研究大鼠血浆中 GRb1 和 GRb1@PLGA@NPs 的药代动力学特征。最佳制备工艺得到的 GRb1@PLGA@NPs 粒径为 120.63nm,多分散指数(PDI)为 0.172,zeta 电位为-22.67mV,包封效率为 75%,载药量为 11%。体外释放显示出持续的药物释放。与 GRb1 相比,GRb1@PLGA@NPs 的达峰时间缩短了约 0.72 倍。血浆浓度-时间曲线下面积显著增加到 GRb1 的 4.58 倍。采用最佳工艺制备的 GRb1@PLGA@NPs 分布均匀,质量稳定,与游离 GRb1 相比,其相对口服生物利用度显著提高。