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通过新型Soluplus-甘草次酸固体分散体提高甘草次酸的生物利用度和抗炎活性

Enhancement of the Bioavailability and Anti-Inflammatory Activity of Glycyrrhetinic Acid via Novel Soluplus-A Glycyrrhetinic Acid Solid Dispersion.

作者信息

Wang Hao, Li Runwei, Rao Yuan, Liu Saixing, Hu Chunhui, Zhang Yong, Meng Linchao, Wu Qilin, Ouyang Qiuhong, Liang Hao, Qin Meng

机构信息

Beijing Advanced Innovation Centre for Soft Matter Science and Engineering, State Key Laboratory of Chemical Resource Engineering, College of Life Science and Technology, Beijing University of Chemical Technology, Beijing 100029, China.

Medical College, Qinghai University, Xining 810001, China.

出版信息

Pharmaceutics. 2022 Aug 26;14(9):1797. doi: 10.3390/pharmaceutics14091797.

DOI:10.3390/pharmaceutics14091797
PMID:36145545
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9504515/
Abstract

Glycyrrhetinic acid (GA) is an anti-inflammatory drug with potential for development. However, the poor solubility of GA in water leads to extremely low bioavailability, which limits its clinical applications. Solid dispersions have become some of the most effective strategies for improving the solubility of poorly soluble drugs. Soluplus, a non-cytotoxic amphiphilic solubilizer, significantly improves the solubility of BCS II drugs and improves the bioavailability of insoluble drugs. l-arginine (L-Arg) can be used as a small molecular weight excipient to assist in improving the solubility of insoluble drugs. In this study, we developed a new formulation for oral administration by reacting GA and L-Arg to form salts by co-solvent evaporation and then adding the polymer-solvent Soluplus with an amphiphilic chemical structure to prepare a solid dispersion GA-SD. The chemical and physical properties of GA-SD were characterized by DLS, TEM, XRD, FT-IR and TG. The anti-inflammatory activity of GA-SD was verified by LPS stimulation of RAW 267.5 cells simulating a cellular inflammation model, TPA-induced ear edema model in mice, and ethanol-induced gastric ulcer model. The results showed that the amide bond and salt formation of GA-SD greatly improved GA solubility. GA-SD effectively improved the anti-inflammatory effect of free GA in vivo and in vitro, and GA-SD had no significant effect on liver and kidney function, no significant tissue toxicity, and good biosafety. In conclusion, GA-SD with L-Arg and Soluplus is an effective method to improve the solubility and bioavailability of GA. As a safe and effective solid dispersion, it is a promising anti-inflammatory oral formulation and provides some references for other oral drug candidates with low bioavailability.

摘要

甘草次酸（GA）是一种具有开发潜力的抗炎药物。然而，GA在水中的溶解度较差，导致其生物利用度极低，这限制了它的临床应用。固体分散体已成为提高难溶性药物溶解度的一些最有效策略。Soluplus是一种无细胞毒性的两亲性增溶剂，能显著提高BCS II类药物的溶解度，并提高难溶性药物的生物利用度。L-精氨酸（L-Arg）可用作小分子辅料，以协助提高难溶性药物的溶解度。在本研究中，我们通过共溶剂蒸发使GA与L-Arg反应形成盐，然后加入具有两亲化学结构的聚合物溶剂Soluplus，开发了一种新的口服制剂，制备了固体分散体GA-SD。通过动态光散射（DLS）、透射电子显微镜（TEM）、X射线衍射（XRD）、傅里叶变换红外光谱（FT-IR）和热重分析（TG）对GA-SD的化学和物理性质进行了表征。通过脂多糖（LPS）刺激RAW 267.5细胞模拟细胞炎症模型、佛波酯（TPA）诱导的小鼠耳部水肿模型和乙醇诱导的胃溃疡模型，验证了GA-SD的抗炎活性。结果表明，GA-SD的酰胺键和盐的形成极大地提高了GA的溶解度。GA-SD在体内外均有效提高了游离GA的抗炎效果，且GA-SD对肝肾功能无显著影响，无明显组织毒性，具有良好的生物安全性。总之，含L-Arg和Soluplus的GA-SD是提高GA溶解度和生物利用度的有效方法。作为一种安全有效的固体分散体，它是一种有前景的抗炎口服制剂，为其他生物利用度低的口服候选药物提供了一些参考。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e71b/9504515/78ca9716e082/pharmaceutics-14-01797-g012.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e71b/9504515/c2045c70de0b/pharmaceutics-14-01797-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e71b/9504515/f52d3fd7e3ee/pharmaceutics-14-01797-g009.jpg
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