Beijing Institute of Technology, Beijing, 100081, PR China; South Subtropical Crop Research Institute, Chinese Academy of Tropical Agricultural Sciences, Zhanjiang, Guangdong 524091, PR China.
South Subtropical Crop Research Institute, Chinese Academy of Tropical Agricultural Sciences, Zhanjiang, Guangdong 524091, PR China.
Colloids Surf B Biointerfaces. 2021 Jun;202:111693. doi: 10.1016/j.colsurfb.2021.111693. Epub 2021 Mar 17.
To increase the solubility and the encapsulation of zinc phthalocyanine (ZnPc) photosensitizer for photodynamic therapy (PDT), a positively charged amphiphilic phosphonium chitosan nanomicelle with multi-benzene structure was developed, and its application to PDT was explored. N-acetyl-l-phenylalanine-(4-carboxybutyl) triphenylphosphonium bromide chitosan (CTPB-CS-NAP), a chitosan derivative with tunable amphiphilicity, was synthesized first. ZnPc was encapsulated in CTPB-CS-NAP at the critical micelle concentration (CMC) of 4.898 mg/L by a hydrophobic self-assembly method to form ZnPc-loaded nanomicelles (ZnPc@CTPB-CS-NAP). The method gives the highest encapsulation efficiency and drug loading of 89.4 % and 22.3 %, respectively. ZnPc@CTPB-CS-NAP is stably dispersed in aqueous solution and shows the average particle size of 103±5 nm. PDT experiments suggest the phototoxicity of ZnPc@CTPB-CS-NAP is much higher than that of ZnPc, but no obvious dark cytotoxicity is observed. Our study has provided a new strategy for improving the photodynamic therapy efficacy of hydrophobic photosensitizer by the encapsulation with chitosan derivative carriers.
为提高锌酞菁（ZnPc）光敏剂用于光动力疗法（PDT）的溶解度和包封率，开发了一种带正电荷的具有多苯结构的两亲性膦酸壳聚糖纳米胶束，并探索了其在 PDT 中的应用。首先合成了具有可调两亲性的壳聚糖衍生物 N-乙酰-L-苯丙氨酸-（4-羧丁基）三苯基溴化膦（CTPB-CS-NAP）。通过疏水自组装法，在临界胶束浓度（CMC）为 4.898mg/L 时，将 ZnPc 包封在 CTPB-CS-NAP 中，形成载 ZnPc 的纳米胶束（ZnPc@CTPB-CS-NAP）。该方法具有最高的包封效率和载药量，分别为 89.4%和 22.3%。ZnPc@CTPB-CS-NAP 在水溶液中稳定分散，平均粒径为 103±5nm。PDT 实验表明，ZnPc@CTPB-CS-NAP 的光毒性明显高于 ZnPc，但未见明显的暗毒性。本研究为通过壳聚糖衍生物载体包封提高疏水性光敏剂的光动力治疗效果提供了一种新策略。
