Preparation, Pharmacokinetics and Anti-Liver Injury Pharmacodynamic Study of Esculin Loaded Liposomes Modified by TPGS

Author:

Shi Feng1,Sun Weigang1,Yin Wenxiong1,Xia Xiaoli1,Adu-Frimpong Michael2,Cao Xia1,Ji Hao3,Wang Qilong1,Xu Ximing1,Yu Jiangnan1

Affiliation:

1. Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu Provincial Research Center for Medicinal Function Development of New Food Resources, Jiangsu University, Zhenjiang, 212013, Jiangsu, China

2. Department of Biochemistry and Forensic Sciences, C. K. Tedam University of Technology and Applied Sciences, Navrongo, 0215-5321, UK, Ghana

3. Jiangsu Tian Sheng Pharmaceutical Co., Ltd., 212415, Zhenjiang, China

Abstract

In this study, Esculin (ES)-loaded liposomes modified with TPGS (ES-TPGS-Ls) were successfully prepared to enhance bioavailability and hepatoprotective activity of this coumarin glucoside. We utilize thin-film dispersion to fabricate ES-TPGS-Ls. The size, polydispersed index (PDI), Zeta potential (Z-potential), morphology, and encapsulation effectiveness of the liposomes were all evaluated afterwards. The storage stability of ES-TPGS-Ls at 4 °C was investigated. The findings showed that ES-TPGS-Ls had spherical nanoparticles with 194.47±8.54 nm as the mean size, 0.239±0.011 as PDI, and −21.16±0.97) mV as Z-potential coupled with encapsulation efficiency (EE) of 91.85±0.44%. Storage stability of liposomes at 4 °C was maintained within one week. Pharmacokinetic study showed that the relative oral bioavailability of ES-TPGS-Ls increased by 2.38 times. Pharmacodynamic studies showed that the developed liposomes could enhance the hepatoprotective activity of ES. Overall, the ES-TPGS-Ls significantly enhanced the bioavailability of esculin, thereby enhancing the in vivo hepatoprotective effect of ES.

Publisher

American Scientific Publishers

Reference48 articles.

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