Journal
CARBOHYDRATE POLYMERS
Volume 92, Issue 1, Pages 545-554Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2012.08.112
Keywords
Chitosan; Paclitaxel; Micelles; Cellular uptake; Tumor targeting
Categories
Funding
- Ph.D. Programs Foundation of Ministry of Education of China [20090096110005]
- 111 Project from the Ministry of Education of China the State Administration of Foreign Expert Affairs of China [111-2-07]
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In this study, a novel amphiphilic copolymer designed as N-octyl-N-phthalyl-3,6-O-(2-hydroxypropyl) chitosan (OPHPC) were synthesized and then conjugated with folic acid (FA-OPHPC) to produce a targeted drug carrier for tumor-specific drug delivery. OPHPC and FA-OPHPC were characterized by FT-IR. H-1 NMR, C-13 NMR and elemental analysis. Paclitaxel (PTX) loaded OPHPC micelles (PTX-OPHPC) with well-defined spherical shape and homogeneous distribution exhibited drug-loading rate ranging from 33.6% to 45.3% and entrapment efficiency from 50.5% to 82.8%. In the cellular uptake studies, PTX-OPHPC brought about a significantly higher amount of PTX accumulated in human breast adenocarcinoma cell line (MCF-7 cells) compared with Taxol (R). Moreover, the cellular uptake of PTX in PTX loaded FA-OPHPC micelles (PTX-FA-OPHPC) was 3.2-fold improved in comparison with that of PTX-OPHPC. The results revealed that OPHPC micelle might be a promising drug carrier for promoting PTX cellular uptake and FA-OPHPC micelle could be used as a potential tumor-targeted drug vector. (C) 2012 Elsevier Ltd. All rights reserved.
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