Zhang Jianghao, Lou Boxuan, Qin Xiaolan, Li Yinwen, Yuan Haikuan, Zhang Lijuan, Liu Xijian, Zhang Yan, Lu Jie
Chemical Engineering Department, Frontier Medical Technologies Institute, Shanghai University of Engineering Science, Shanghai 201620, China.
Materials Science & Engineering School, Linyi University, Linyi 276000, China.
ACS Omega. 2022 Jun 7;7(24):21000-21013. doi: 10.1021/acsomega.2c01792. eCollection 2022 Jun 21.
Biocompatible and biodegradable amphiphilic polymeric micelles (PLA-CMCS-g-OA) were prepared by surface grafting of oleic acid and polylactic acid onto carboxymethyl chitosan and were used as templates for the crystallization of camptothecin. The camptothecin (CPT) nanocrystals prepared by the novel micelle-templated antisolvent crystallization (mt-ASC) method demonstrated higher crystallinity, narrower particle size distribution, and slower release characteristic than those prepared by conventional antisolvent crystallization (c-ASC) using a high initial concentration and fast addition rate. In particular, the CPT release behavior of mt-ASC products in phosphate buffer solutions presented a pH-responsive characteristic with the increasing release rate of CPT under lower pH conditions. This work confirmed that amphiphilic nanomicelle-templated crystallization was an effective method for preparing drug nanocrystals.
通过将油酸和聚乳酸接枝到羧甲基壳聚糖表面制备了具有生物相容性和可生物降解性的两亲性聚合物胶束（PLA-CMCS-g-OA），并将其用作喜树碱结晶的模板。通过新型胶束模板抗溶剂结晶（mt-ASC）方法制备的喜树碱（CPT）纳米晶体比使用高初始浓度和快速添加速率的传统抗溶剂结晶（c-ASC）方法制备的纳米晶体具有更高的结晶度、更窄的粒径分布和更慢的释放特性。特别是，mt-ASC产物在磷酸盐缓冲溶液中的CPT释放行为呈现出pH响应特性，在较低pH条件下CPT的释放速率增加。这项工作证实了两亲性纳米胶束模板结晶是制备药物纳米晶体的有效方法。
