Center for Molecular Science and Engineering, College of Science, Northeastern University, Shenyang, 110819, People's Republic of China.
Fujian Key Laboratory of Toxicant and Drug Toxicology, Medical College, Ningde Normal University, Ningde, Fujian, 352100, People's Republic of China.
Drug Deliv Transl Res. 2023 Sep;13(9):2394-2406. doi: 10.1007/s13346-023-01323-w. Epub 2023 Mar 13.
Enhancing tissue permeability and achieving drug aggregation is the key to targeted tumor therapy. A series triblock copolymers of poly(ethylene glycol)-poly(L-lysine)-poly(L-glutamine) were synthesized by ring-opening polymerization, and charge-convertible nano-delivery system was constructed by loading doxorubicin (DOX) with 2-(hexaethylimide) ethanol on side chain. In normal environment (pH = 7.4), the zeta potential of the drug-loaded nanoparticle solution is negative, which is conducive to avoiding the identification and clearance of nanoparticles by the reticulo-endothelial system, while potential-reversal can be achieved in the tumor microenvironment, which effectively promotes cellular uptake. Nanoparticles could effectively reduce the distribution of DOX in normal tissues and achieve targeted aggregation at tumor sites, which can effectively improve the antitumor effect, while would not causing toxicity and damage to normal body.
增强组织通透性和实现药物聚集是靶向肿瘤治疗的关键。通过开环聚合合成了一系列聚乙二醇-聚 L-赖氨酸-聚 L-谷氨酰胺嵌段共聚物，并通过在侧链上用 2-(己基咪唑)乙醇装载阿霉素 (DOX) 构建了可转换电荷的纳米递药系统。在正常环境 (pH = 7.4) 下，载药纳米颗粒溶液的zeta 电位为负，有利于避免纳米颗粒被网状内皮系统识别和清除，而在肿瘤微环境中可以实现电位反转，从而有效促进细胞摄取。纳米颗粒可以有效减少 DOX 在正常组织中的分布，并在肿瘤部位实现靶向聚集，从而有效提高抗肿瘤效果，同时不会对正常身体造成毒性和损伤。
