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通过巯基化三甲基壳聚糖和麦胚凝集素修饰的纳米制剂促进三七总皂苷的口服吸收。

Promoting oral absorption of Panax notoginseng saponins via thiolated trimethyl chitosan and wheat germ agglutinin-modified nanoformulation.

机构信息

College of Pharmacy, Guilin Medical University, No. 1 Zhiyuan Road, Guilin, 541199, People's Republic of China.

Pharmacology Laboratory of Prevention and Treatment of High Incidence of Disease, Guilin Medical University, Guilin, 541104, People's Republic of China.

出版信息

Drug Deliv Transl Res. 2024 Mar;14(3):621-636. doi: 10.1007/s13346-023-01417-5. Epub 2023 Oct 3.

Abstract

This study aimed to enhance the oral absorption of Panax notoginseng saponins (PNS) via nanoparticles modified with thiolated trimethyl chitosan (TMC-Cys) and wheat germ agglutinin (WGA), termed PP-WT NPs. In vitro investigations revealed that PP-WT NPs exhibited delayed release of PNS and a strong tolerance to the gastric acids and digestive enzymes. Moreover, PP-WT NPs exhibited efficient cellular uptake and transport capabilities in the Caco-2/HT29-co-cultured cell model. In vivo animal experiments demonstrated that PP-WT NPs effectively overcame the mucus layer barrier, with the effective permeability coefficients of R1, Rg1, and Rb1 in the small intestine being 1.68, 1.64, and 1.63 times higher than those of free PNS, respectively. Taken together, thiolated trimethyl chitosan and wheat germ agglutinin-modified nanoparticles hold significant potential for improving the oral absorption of PNS, representing an attractive strategy for enhanced therapeutic efficacy.

摘要

本研究旨在通过用巯基化三甲基壳聚糖(TMC-Cys)和麦胚凝集素(WGA)修饰的纳米粒来提高三七总皂苷(PNS)的口服吸收,称为 PP-WT NPs。体外研究表明,PP-WT NPs 表现出 PNS 的延迟释放和对胃酸和消化酶的强耐受性。此外,PP-WT NPs 在 Caco-2/HT29 共培养细胞模型中表现出有效的细胞摄取和转运能力。体内动物实验表明,PP-WT NPs 能有效克服黏液层屏障,小肠中 R1、Rg1 和 Rb1 的有效渗透系数分别比游离 PNS 高 1.68、1.64 和 1.63 倍。综上所述,巯基化三甲基壳聚糖和麦胚凝集素修饰的纳米粒具有显著提高 PNS 口服吸收的潜力,为增强治疗效果提供了一种有吸引力的策略。

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