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采用 和 模型评估乳化川陈皮素的口服生物利用度和生物转化。

Assessment of Oral Bioavailability and Biotransformation of Emulsified Nobiletin Using and Models.

机构信息

Department of Food Science, Rutgers University, 65 Dudley Road, New Brunswick 08901, New Jersey, United States.

Guangdong Provincial Key Laboratory of Nutraceuticals and Functional Foods, College of Food Science, South China Agricultural University, Guangzhou 510642, Guangdong, China.

出版信息

J Agric Food Chem. 2020 Oct 14;68(41):11412-11420. doi: 10.1021/acs.jafc.0c04450. Epub 2020 Sep 30.

DOI:10.1021/acs.jafc.0c04450
PMID:32935545
Abstract

Nobiletin has received much attention for its promising biological activities. Owing to its limited solubility, various encapsulation strategies have been developed to enhance nobiletin bioavailability. However, the understanding of the bioavailability and biotransformation of nobiletin and the correlation between and data remains limited. This study developed a high-loading nobiletin (1%) emulsion. The models, which combined pH-stat lipolysis with a Franz cell, showed very good correlation with data for the relative bioavailability. Rat studies showed that nobiletin had a high absolute bioavailability (≈20% for oil suspension). Besides, the emulsification improved the amount of bioavailable nobiletin and its major metabolite in the blood by about two times, as compared to an oil suspension. This work provides scientific insights into a rapid screening method for delivery systems and a better understanding of the biological fate of nobiletin .

摘要

川陈皮素因其有前景的生物活性而受到广泛关注。由于其溶解度有限,已经开发了各种包封策略来提高川陈皮素的生物利用度。然而,对于川陈皮素的生物利用度和生物转化的理解以及 和 数据之间的相关性仍然有限。本研究开发了一种高载量的川陈皮素(1%)乳剂。结合 pH -stat 脂肪酶解和 Franz 室的 模型与 数据显示出非常好的相关性,表明相对生物利用度较高。大鼠研究表明,川陈皮素的绝对生物利用度很高(油混悬液约为 20%)。此外,与油混悬液相比,乳化作用使血液中可利用的川陈皮素及其主要代谢物的量增加了约两倍。这项工作为快速筛选输送系统提供了科学见解,并更好地理解了川陈皮素的生物命运。

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