State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, People's Republic of China.
State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, People's Republic of China.
Int J Biol Macromol. 2019 Dec 1;141:161-170. doi: 10.1016/j.ijbiomac.2019.08.251. Epub 2019 Aug 31.
Core-shell-corona chitosan-based micelles were designed for the tumor intracellular pH-triggered doxorubicin (DOX) delivery, via a facile in-situ micellization in an aqueous solution of DOX and polyethylene glycol (PEG) and poly(2-(diisopropylamino) ethyl methacrylate) (PDPA) dual-modified chitosan (PEG-g-CS-g-PDPA). The effect of the PDPA modification on the diameter, drug loading-capacity (DLC) and pH-triggered drug release was investigated for the three different polymerization degrees of PDPA (25, 32, and 42) with a similar modification degree of ~22%. The optimized ones, the core-shell-corona DOX/PEG-g-CS-g-PDPA micelles possessed a mean hydrodynamic diameter (D) of 211 nm and DLC of 54%, showing an excellent pH-triggered drug release with negligible premature drug leakage in 60 h. Such results indicated that grafting polycation could efficiently improve the performance of the chitosan-based drug delivery system (DDS) for tumor chemotherapy.
基于壳核冠壳结构的壳聚糖胶束被设计用于肿瘤细胞内 pH 触发的阿霉素（DOX）递送，通过在 DOX 和聚乙二醇（PEG）和聚（2-（二异丙基氨基）乙基甲基丙烯酸酯）（PDPA）双重修饰的壳聚糖（PEG-g-CS-g-PDPA）的水溶液中进行简便的原位胶束化来实现。研究了 PDPA 聚合度为 25、32 和 42 的三种不同聚合度对胶束粒径、载药量（DLC）和 pH 触发药物释放的影响，其相似的修饰度约为 22%。优化后的 DOX/PEG-g-CS-g-PDPA 核壳冠胶束的平均水动力直径（D）为 211nm，载药量（DLC）为 54%，在 60h 内具有优异的 pH 触发药物释放性能，几乎没有早期药物泄漏。这些结果表明，接枝聚阳离子可以有效地提高基于壳聚糖的药物递送系统（DDS）用于肿瘤化疗的性能。
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