Novel pH-sensitive chitosan-derived micelles loaded with paclitaxel
Novel pH-sensitive chitosan-derived micelles loaded with paclitaxel
复制标题
负载紫杉醇的新型 pH 敏感壳聚糖衍生胶束
DOI：
10.1016/j.carbpol.2010.04.084
复制
发表时间：
2010-09-05
影响因子：
11.2
通讯作者：
Ping, Qineng
中科院分区：
文献类型：
--
作者：
Liu, Jia;Li, Hongxia;Ping, Qineng
合成了一系列pH敏感性接枝共聚物N-辛基-N-（2-羧基-环己亚甲基）壳聚糖衍生物，用FTIR、H-1 NMR和元素分析对其进行了表征，并用差示扫描量热法和X射线衍射法对其物理性能进行了测定。以芘为疏水探针，用荧光光谱法测得改性壳聚糖的临界胶束浓度（CMC）为11 ~ 72 μ g/ml。该接枝聚合物可形成增溶紫杉醇的胶束，载药率为30.47%~ 48.10%，包封率为42.22%~ 59.24%。载体对肿瘤细胞的细胞毒性估计载体几乎无细胞毒性。此外，pH敏感性和药物释放实验的结果表明，胶束是高度敏感的弱酸性条件（pH 5.5），而在生理条件下（pH 7.4）相当稳定。因此，壳聚糖衍生胶束有望成为一种潜在的抗肿瘤化疗药物载体。(C)2010爱思唯尔有限公司保留所有权利。
A series of pH-sensitive graft copolymers, N-octyl-N-(2-carboxyl-cyclohexamethenyl) chitosan derivatives were synthesized and characterized by FTIR, H-1 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 mu g/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. (C) 2010 Elsevier Ltd. All rights reserved.