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两亲性 PEG 化药物自组装胶束用于癌症治疗。

Self-Assembled Micelles of Amphiphilic PEGylated Drugs for Cancer Treatment.

机构信息

School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China.

Department of Interventional Radiology, Ruijin Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China.

出版信息

Curr Drug Targets. 2021;22(8):870-881. doi: 10.2174/1389450122666201231130702.

Abstract

Generally, poor solubility and imprecise delivery of chemotherapeutic drugs can compromise their efficacies for clinical cancer treatment. In order to address such concerns, poor water-soluble drugs are conjugated with poly(ethylene glycol) (PEG) to obtain PEGylated drugs, which have improved water solubility and can also self-assemble in an aqueous solution to form micelles (PEGylated drug micelles). The surface PEG layer enhances the micelles' colloidal stability and reduces the interaction with physiological surroundings. Meanwhile, PEGylated drug micelles are tumor- targeting via the enhanced permeation and retention (EPR) effect to improve antitumor efficacy in comparison with free drugs. PEGylated drug micelles employ drugs as parts of the carrier medium, which increases the micelles' drug loading capacity relatively. The development of stimuli- responsive PEGylated drug micelles facilitates the drug release to be smart and controllable. Moreover, the PEGylated drug micelles show great potentials in overcoming the challenges of cancer therapy, such as multidrug resistance (MDR), angiogenesis, immunosuppression, and so on. In this review, we highlight the research progresses of PEGylated drug micelles, including the structures and properties, smart stimuli-responsive PEGylated drug micelles, and the challenges that have been overcome by PEGylated drug micelles.

摘要

一般来说,化疗药物溶解度差和给药不准确会影响其临床癌症治疗效果。为了解决这些问题,将水溶性差的药物与聚乙二醇(PEG)连接,得到PEG 化药物,提高了水溶性,也可以在水溶液中自组装形成胶束(PEG 化药物胶束)。PEG 层增加了胶束的胶体稳定性并减少了与生理环境的相互作用。同时,PEG 化药物胶束通过增强的渗透和保留(EPR)效应靶向肿瘤,与游离药物相比,提高了抗肿瘤疗效。PEG 化药物胶束将药物作为载体介质的一部分,相对增加了胶束的载药量。刺激响应型 PEG 化药物胶束的发展促进了药物释放的智能化和可控化。此外,PEG 化药物胶束在克服癌症治疗中的多重耐药性(MDR)、血管生成、免疫抑制等挑战方面具有巨大的潜力。在这篇综述中,我们强调了 PEG 化药物胶束的研究进展,包括结构和性质、智能刺激响应型 PEG 化药物胶束以及 PEG 化药物胶束克服的挑战。

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