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纳米乳剂提高橙皮苷口服生物利用度的研究:制剂优化及吸收机制。

Nanoemulsion for Improving the Oral Bioavailability of Hesperetin: Formulation Optimization and Absorption Mechanism.

机构信息

School of Pharmaceutical Sciences, Chongqing University, Chongqing, 401331, China.

School of Pharmaceutical Sciences, Chongqing University, Chongqing, 401331, China.

出版信息

J Pharm Sci. 2021 Jun;110(6):2555-2561. doi: 10.1016/j.xphs.2021.02.030. Epub 2021 Feb 27.

Abstract

This study aimed to prepare a nanoemulsion vehicle to improve the oral bioavailability of hesperetin. The pseudo-ternary phase diagrams and the RSM were used to optimize nanoemulsion parameters. Compared with hesperetin suspension, the AUC and C of nanoemulsion were increased by 5.67-fold and 2.64-fold, respectively. The proportion of lymphatic transport reached 87.72%, the cumulative absorption amount of jejunum, ileum, and duodenum increased by 1.1-fold, 1.92-fold, and 1.5-fold, respectively. The results implied that hesperetin nanoemulsion could effectively improve the bioavailability of hesperetin by increasing lymphatic transport and enhancing intestinal permeability. Therefore, nanoemulsion is a potential method to improve the bioavailability of hesperetin, which has strong practicability.

摘要

本研究旨在制备纳米乳载体以提高橙皮苷的口服生物利用度。采用伪三元相图和响应面法优化纳米乳参数。与橙皮苷混悬液相比,纳米乳的 AUC 和 C 分别增加了 5.67 倍和 2.64 倍。淋巴转运比例达到 87.72%,空肠、回肠和十二指肠的累积吸收量分别增加了 1.1 倍、1.92 倍和 1.5 倍。结果表明,橙皮苷纳米乳可通过增加淋巴转运和增强肠道通透性有效提高橙皮苷的生物利用度。因此,纳米乳是提高橙皮苷生物利用度的一种有潜力的方法,具有很强的实用性。

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