School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, 30 Qingquan Road, Yantai, 264005, Shandong, People's Republic of China.
State Key Laboratory of Long-Acting and Targeting Drug Delivery System, Shandong Luye Pharmaceutical Co. Ltd, Yantai, 264003, People's Republic of China.
J Nanobiotechnology. 2022 Jan 10;20(1):31. doi: 10.1186/s12951-021-01221-8.
Surface charge of biological and medical nanocarriers has been demonstrated to play an important role in cellular uptake. Owing to the unique physicochemical properties, charge-reversal delivery strategy has rapidly developed as a promising approach for drug delivery application, especially for cancer treatment. Charge-reversal nanocarriers are neutral/negatively charged at physiological conditions while could be triggered to positively charged by specific stimuli (i.e., pH, redox, ROS, enzyme, light or temperature) to achieve the prolonged blood circulation and enhanced tumor cellular uptake, thus to potentiate the antitumor effects of delivered therapeutic agents. In this review, we comprehensively summarized the recent advances of charge-reversal nanocarriers, including: (i) the effect of surface charge on cellular uptake; (ii) charge-conversion mechanisms responding to several specific stimuli; (iii) relation between the chemical structure and charge reversal activity; and (iv) polymeric materials that are commonly applied in the charge-reversal delivery systems.
生物和医学纳米载体的表面电荷已被证明在细胞摄取中起着重要作用。由于具有独特的物理化学性质，电荷反转递药策略作为一种很有前途的药物递送应用方法，特别是在癌症治疗方面，迅速得到了发展。在生理条件下，电荷反转纳米载体呈中性/负电性，但可以通过特定刺激（即 pH 值、氧化还原、ROS、酶、光或温度）触发转变为正电性，从而实现延长血液循环和增强肿瘤细胞摄取，从而增强递药治疗剂的抗肿瘤效果。在这篇综述中，我们全面总结了电荷反转纳米载体的最新进展，包括：（i）表面电荷对细胞摄取的影响；（ii）响应几种特定刺激的电荷转换机制；（iii）化学结构与电荷反转活性之间的关系；和（iv）常用于电荷反转递药系统的聚合物材料。
