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Novel pH-sensitive chitosan-derived micelles loaded with paclitaxel

Authors
Journal
Carbohydrate Polymers
0144-8617
Publisher
Elsevier
Publication Date
Volume
82
Issue
2
Identifiers
DOI: 10.1016/j.carbpol.2010.04.084
Keywords
  • Chitosan Derivatives
  • Ph-Sensitive
  • Polymeric Micelles
  • Paclitaxel
Disciplines
  • Biology
  • Medicine

Abstract

Abstract A series of pH-sensitive graft copolymers, N-octyl- N-(2-carboxyl-cyclohexamethenyl) chitosan derivatives were synthesized and characterized by FTIR, 1H NMR and elemental analysis, and their physical properties were measured with differential scanning calorimetry and X-ray diffraction spectrometry. The critical micelle concentrations (CMCs) of the modified chitosan determined by using pyrene as a hydrophobic probe in fluorescence spectroscopy were from 11 to 72 μg/ml. The graft polymers can form micelles solubilizing paclitaxel, with drug-loading rate ranging from 30.47% to 48.10% and entrapment efficiency from 42.22% to 59.24%. Cytotoxicities of carrier against tumor cells estimated that carriers were nearly non-cytotoxic. Additionally, the results of pH-sensitivity and drug release experiments showed that the micelles were highly sensitive to mild acidic conditions (pH 5.5) while reasonably stable at physiological conditions (pH 7.4). Therefore, chitosan-derived micelle may be a potential anti-tumor drug delivery system for chemotherapy of cancer.

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