Wu Zhenyao, Li Jie, Zhang Xin, Li Yangjia, Wei Dongwei, Tang Lichang, Deng Shiming, Liu Guijin
School of Pharmaceutical Sciences, Hainan University, Haikou 570100, China.
School of Chemical Engineering and Materials Science, Quanzhou Normal University, Quanzhou 362000, China.
ACS Omega. 2022 Apr 7;7(15):13371-13381. doi: 10.1021/acsomega.2c01270. eCollection 2022 Apr 19.
The objective of this work is to design and fabricate a natural zein-based nanocomposite with core-shell structure for the delivery of anticancer drugs. As for the design, folate-conjugated zein (Fa-zein) was synthesized as the inner hydrophobic core; soy lecithin (SL) and carboxymethyl chitosan (CMC) were selected as coating components to form an outer shell. As for fabrication, a novel and appropriate atomizing/antisolvent precipitation process was established. The results indicated that Fa-zein/SL/CMC core-shell nanoparticles (FZLC NPs) were successfully produced at a suitable mass ratio of Fa-zein/SL/CMC (100:30:10) and the freeze-dried FZLC powder showed a perfect redispersibility and stability in water. After that, docetaxel (DTX) as a model drug was encapsulated into FZLC NPs at different mass ratios of DTX to FZLC (). When = 1:15, DTX/FZLC NPs were obtained with high encapsulation efficiency (79.22 ± 0.37%), small particle size (206.9 ± 48.73 nm), and high zeta potential (-41.8 ± 3.97 mV). DTX was dispersed in the inner core of the FZLC matrix in an amorphous state. The results proved that DTX/FZLC NPs could increase the DTX dissolution, sustain the DTX release, and enhance the DTX cytotoxicity significantly. The present study provides insight into the formation of zein-based complex nanocarriers for the delivery of anticancer drugs.
本研究的目的是设计并制备一种具有核壳结构的天然玉米醇溶蛋白基纳米复合材料，用于抗癌药物的递送。在设计方面，合成了叶酸共轭玉米醇溶蛋白（Fa-zein）作为内部疏水核心；选择大豆卵磷脂（SL）和羧甲基壳聚糖（CMC）作为涂层成分以形成外壳。在制备方面，建立了一种新颖且合适的雾化/抗溶剂沉淀工艺。结果表明，在Fa-zein/SL/CMC质量比为100:30:10时成功制备了Fa-zein/SL/CMC核壳纳米颗粒（FZLC NPs），冻干的FZLC粉末在水中表现出良好的再分散性和稳定性。之后，将多西他赛（DTX）作为模型药物以不同的DTX与FZLC质量比封装到FZLC NPs中（）。当 = 1:15时，获得了具有高包封率（79.22 ± 0.37%）、小粒径（206.9 ± 48.73 nm）和高zeta电位（-41.8 ± 3.97 mV）的DTX/FZLC NPs。DTX以无定形状态分散在FZLC基质的内核中。结果证明，DTX/FZLC NPs可显著提高DTX的溶解度、维持DTX的释放并增强DTX的细胞毒性。本研究为基于玉米醇溶蛋白的复合纳米载体用于抗癌药物递送的形成提供了见解。
