期刊
CARBOHYDRATE POLYMERS
卷 206, 期 -, 页码 121-131出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2018.10.096
关键词
Polymeric micelles; Oral delivery; Carboxymethyl chitosan; Rhein; Paclitaxel; Synergistic antitumor effect
资金
- National Natural Science Foundation of China [81603301]
- Project Program of Fujian Provincial Department of Science and Technology [2015Y0064]
- Fujian Key Laboratory of Chinese Materia Medica
- Personnel Training Funding of Fujian Province Health Department [2016-ZQN-69]
- Program for New Century Excellent Talents in Fujian Province University [23]
- Overseas studies scholarship in Fujian province
An amphiphilic carboxymethyl chitosan-rhein (CR) conjugate was prepared, characterized, and evaluated as a potential carrier material for oral delivery of paclitaxel (PTX). CR conjugate self-assembled in aqueous environment into CR polymeric micelles (CR PMs). The drug loading capacity and entrapment efficiency of PTX-loaded CR PMs were 35.24 +/- 1.58% and 86.99 +/- 12.26%, respectively. Pharmacokinetic results indicate that PTX-loaded CR PMs could significantly enhance the oral bioavailability of PTX. Confocal imaging of intestinal sections verified many of CR PMs were absorbed as whole through the intestinal membrane. The cytotoxicity assays in Caco-2 cells and in vivo antitumor efficacy showed that PTX-loaded CR PMs had a stronger antitumor efficacy. A synergistic antitumor effect between CR conjugate and PTX was proven in MCF-7 cells and antitumor efficacy studies. The investigation of CR conjugate developed in this study showed that CR PMs are promising for oral delivery of water-insoluble antitumor drugs.
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