Preparation of N-alkyl-O-sulfate chitosan derivatives and micellar solubilization of taxol

Preparation of N-alkyl-O-sulfate chitosan derivatives and micellar solubilization of taxol
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DOI:
10.1016/s0144-8617(03)00090-0
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发表时间:
2003-11-01
影响因子:
11.2
通讯作者:
Jian, S
Jian, S
中科院分区:
化学1区
文献类型:
--
作者:
Can, Z;Ping, QN;Jian, S

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合成了一系列新型壳聚糖衍生物,它们分别含有长链烷基(n = 8,10,12)作为疏水基团和硫酸化基团作为亲水基团。用元素分析、红外光谱、核磁共振氢谱和核磁共振碳谱对壳聚糖衍生物的化学结构进行了表征。用TG和WAXD对壳聚糖衍生物的物理性能进行了测试。由该衍生物在水中形成尺寸约为100-400 nm的聚合物胶束。紫杉醇是一种水不溶性的抗癌药物,通过物理包埋将其增溶到聚合物胶束中。结果表明,在N-辛基-O-硫酸酯壳聚糖(OCS 1)胶束溶液中紫杉醇的浓度为2.01 mg/ml,远高于水溶液中紫杉醇的浓度(
A series of novel chitosan derivative carrying long chain alkyl groups (n = 8, 10, 12) as hydrophobic moieties and sulfated groups as hydrophilic moieties were synthesized. The chemical structure of chitosan derivatives were characterized by elemental analysis, FTIR, H-1 NMR and C-13 NMR. Some physical properties of chitosan derivative were measured by TG and WAXD. Polymeric micelles of size around 100-400 nm were formed in water from the derivative. Taxol, a water insoluble anticancer drug, was solubilized into the polymeric micelle by physical entrapment. The result shows that the taxol concentration in the N-octyl-O-sulfate chitosan (OCS1) micellar solution was 2.01 mg/ml, which was much higher than that in water (