Preparation and characterization of self-assembled nanoparticles of 6-O-cholesterol-modified chitosan for drug delivery
Preparation and characterization of self-assembled nanoparticles of 6-O-cholesterol-modified chitosan for drug delivery
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用于药物输送的 6-O-胆固醇修饰壳聚糖自组装纳米粒子的制备和表征
DOI：
10.1016/j.carbpol.2011.01.012
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发表时间：
2011-04-02
影响因子：
11.2
通讯作者：
Zhang, Qiqing
中科院分区：
文献类型：
--
作者：
Chen, Mingmao;Liu, Yan;Zhang, Qiqing
以邻苯二甲酰化壳聚糖为中间体，通过保护-接枝-脱保护的方法合成了6-O-胆固醇修饰的琥珀酰化壳聚糖（O-CHCS）。通过傅里叶变换红外光谱（FTIR）和质子核磁共振（H-1 NMR）对O-CHCS偶联物进行了表征，并通过元素分析测定了胆固醇部分的取代度（DS）分别为1.7%、4.0%和5.9%。透析法制备的O-CHCS自组装纳米粒子具有典型的“核-壳”结构，粒径在100-240 nm之间。以全反式维甲酸（ATRA）为模型药物，采用透析法将ATRA物理包埋在O-CHCS自组装纳米粒中。随着药物初始含量的增加，载药量增加，但包封率和粒径减小。体外释药曲线表明，ATRA在72 h内缓慢缓释，表明O-CHCS自组装纳米粒具有作为疏水性药物载体的潜力。(C)2011爱思唯尔有限公司保留所有权利。
6-O-Cholesterol modified chitosan (O-CHCS) conjugates with succinyl linkages were synthesized through a protection-graft-deprotection method with phthaloylchitosan as an intermediate. O-CHCS conjugates were characterized by Fourier transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (H-1 NMR), and the degrees of substitution (DS) of the cholesterol moiety determined by elemental analysis were 1.7%, 4.0% or 5.9%. O-CHCS self-assembled nanoparticles prepared by the dialysis method displayed the classic "core-shell" structures and their sizes were in the range of 100-240 nm. All-trans retinoic acid (ATRA), as a model drug, was physically entrapped inside O-CHCS self-assembled nanoparticles by the dialysis method. With increasing initial levels of the drug, the drug loading content increased, but the encapsulation efficiency and the particle size decreased. The release profiles in vitro demonstrated that ATRA showed slow sustained released over 72 h, which indicated that O-CHCS self-assembled nanoparticles had the potential to be used as a carrier for hydrophobic drugs. (C) 2011 Elsevier Ltd. All rights reserved.