Journal
CARBOHYDRATE POLYMERS
Volume 215, Issue -, Pages 8-19Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.carbpol.2019.03.064
Keywords
Paclitaxel; Redox-sensitive; Retinoic acid; Polymeric micelles; Chitosan
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Funding
- Shandong Provincial Natural Science Foundation, China [ZR2017LC010]
- project of Shandong Province Higher Educational Science and Technology Program [J17KA001]
- National Natural Science Foundation of China [81703391]
- National College Students' innovation and entrepreneurship training program of China [201710440117]
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Novel chitosan-cystamine-retinoic acid conjugate (CS-SS-RA) was synthesized and could self-assemble into redox-sensitive micelles in aqueous environment with low critical micelle concentration value. CS-SS-RA micelles were characterized with spherical shape, desirable particle size, negative zeta potential, high paclitaxel (PTX) loading and encapsulation efficiency and redox-sensitivity. Hemolysis and cytotoxicity studies proved the safety of CS-SS-RA micelles for intravenous administration. Cytotoxicity study against HepG2 cells and the growth inhibition study on three-dimensional multicellular tumor spheroids (MCTSs) revealed that PTX-loaded CS-SS-RA micelles exhibited higher antitumor activity than free PTX. The in vitro cellular uptake profiles of FITC-labeled CS-SS-RA micelles evaluated via confocal laser scanning microscopy and flow cytometry indicated that CS-SS-RA micelles could enhance cellular uptake efficiency of PTX, and their internalization by HepG2 cells were mediated by clathrin-mediated endocytosis and macropinocytosis. These results demonstrated that CS-SS-RA micelles could be developed as a promising platform for intracellular delivery of hydrophobic antitumor agents.
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