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TPGS 修饰杨梅素混合胶束的表征、药代动力学和组织分布研究。

The characterisation, pharmacokinetic and tissue distribution studies of TPGS modified myricetrin mixed micelles in rats.

机构信息

a Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering , Jiangsu University , Zhenjiang , China.

b Jiangsu Provincial Research Center for Medicinal Function Development of New Food Resources , Zhenjiang , P.R. China.

出版信息

J Microencapsul. 2019 May;36(3):278-290. doi: 10.1080/02652048.2019.1622606. Epub 2019 Jun 7.

Abstract

This study was designed to investigate the bioavailability and targeting of myricetrin-loaded ternary micelles modified with and without TPGS. The particle diameters of myricetrin-loaded micelles and myricetrin-loaded-TPGS micelle were 30.93 ± 1.34 nm and 26.42 ± 0.89 nm, respectively, while their respective encapsulation efficiencies (m/m, %) were 83.3 ± 1.08 and 93.8 ± 1.18. The release rate of myricetrin in the micellar system clearly exceeded the free myricetrin in the three media (pH 6.8 phosphate buffer, pH 1.2 HCl solution and double distilled water). studies displayed that the bioavailability of myricetrin mixed micelles was remarkably improved than the free drug after oral administration. Moreover, the results of tissue distribution showed that myricetrin-loaded-TPGS micelles accumulated well in the liver tissue. Based on these results, it was speculated that myricetrin-loaded-TPGS micelles might act as a promising carrier for liver targeting with improved hepatic concentration of myricetrin compared with the myricetrin-loaded micelles.

摘要

本研究旨在考察负载杨梅素的三元胶束的生物利用度和靶向性,这些胶束分别经过和未经 TPGS 修饰。负载杨梅素的胶束和负载杨梅素-TPGS 胶束的粒径分别为 30.93±1.34nm 和 26.42±0.89nm,其各自的包封率(m/m,%)分别为 83.3±1.08 和 93.8±1.18。胶束系统中杨梅素的释放率明显高于三种介质(pH6.8 磷酸盐缓冲液、pH1.2 HCl 溶液和双蒸水)中游离杨梅素的释放率。研究表明,口服负载杨梅素混合胶束后,其生物利用度明显高于游离药物。此外,组织分布研究结果表明,负载 TPGS 的杨梅素胶束在肝组织中蓄积良好。基于这些结果,可以推测负载 TPGS 的杨梅素胶束可能作为一种有前途的肝靶向载体,与负载杨梅素的胶束相比,其杨梅素在肝脏中的浓度有所提高。

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