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人参皂苷 Rb1-PLGA 纳米粒的制备、表征及体内药代动力学研究。

Preparation, characterization and in vivo pharmacokinetic study of ginsenoside Rb1-PLGA nanoparticles.

机构信息

College of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, China.

College of Chinese Medicine, Hunan University of Chinese Medicine, Changsha, 410208, China.

出版信息

Sci Rep. 2023 Oct 27;13(1):18472. doi: 10.1038/s41598-023-45858-x.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8706/10611732/a740093498f3/41598_2023_45858_Fig1_HTML.jpg

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