In vitro and in vivo performance of amorphous solid dispersions of ursolic acid as a function of polymer type and excipient addition.

IF 2.8 4区医学 Q2 PHARMACOLOGY & PHARMACY

Journal of Pharmacy and Pharmacology Pub Date : 2024-10-11 DOI:10.1093/jpp/rgae125

Tingting Zhao, Chenming Gu, Jianbo Qi, Jingwen Liu, Yajun Wang, Xiaojing Chen, Fujiang Guo, Yiming Li

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引用次数: 0

Abstract

Objectives: The objective of this research was to enhance the bioavailability of ursolic acid (UA) by preparing multielement amorphous solid dispersion (ASD) systems comprising excipients.

Methods: The ASDs were prepared via the solvent evaporation method, characterized by a range of techniques, and investigated with respect to permeability of human colorectal adenocarcinoma cell line (Caco-2) cells monolayers and pharmacokinetics, with comparisons made to the physical mixture and the pure drug.

Key findings: The (UA-choline)-Polyethylcaprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer (Soluplus)-Vitamin E polyethylene glycol succinate (TPGS) ASD demonstrated superior dissolution properties compared to the corresponding binary solid dispersions and ternary solid dispersions (P < .05). The permeability studies of Caco-2 cell monolayers revealed that the ASD exhibited moderate permeability, with an efflux rate that was significantly lower than that of the UA raw material (P < .05). Pharmacokinetic studies in rats demonstrated that the oral bioavailability of the ASD was 19.0 times higher than that of UA (P < .01).

Conclusions: The research indicated that the multielement ASD could be employed as an efficacious drug delivery system for UA. Furthermore, the Soluplus/TPGS/choline combination represents a promising candidate for the fabrication of ASDs that can load weakly acidic and poorly soluble drugs.

查看原文本刊更多论文

熊果酸无定形固体分散体的体外和体内性能与聚合物类型和辅料添加量的关系。

研究目的本研究旨在通过制备包含辅料的多元素无定形固体分散体（ASD）系统来提高熊果酸（UA）的生物利用度：方法：通过溶剂蒸发法制备无定形固体分散体，采用一系列技术对其进行表征，并研究其在人结肠直肠腺癌细胞系（Caco-2）细胞单层中的渗透性和药代动力学，同时与物理混合物和纯药物进行比较：主要发现：与相应的二元固体分散体和三元固体分散体相比，（UA-胆碱）-聚乙基己内酰胺-聚乙酸乙烯酯-聚乙二醇接枝共聚物（Soluplus）-维生素E聚乙二醇琥珀酸酯（TPGS）ASD表现出更优越的溶解性能（P结论）：研究表明，多元素 ASD 可用作 UA 的有效给药系统。此外，Soluplus/TPGS/胆碱组合是制造可负载弱酸性和难溶性药物的 ASD 的理想候选材料。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Pharmacy and Pharmacology 医学-药学

CiteScore

6.60

自引率

0.00%

发文量

审稿时长

3 months

期刊介绍： JPP keeps pace with new research on how drug action may be optimized by new technologies, and attention is given to understanding and improving drug interactions in the body. At the same time, the journal maintains its established and well-respected core strengths in areas such as pharmaceutics and drug delivery, experimental and clinical pharmacology, biopharmaceutics and drug disposition, and drugs from natural sources. JPP publishes at least one special issue on a topical theme each year.