Cleavable PEGylation: a strategy for overcoming the "PEG dilemma" in efficient drug delivery.
Cleavable PEGylation: a strategy for overcoming the "PEG dilemma" in efficient drug delivery.
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可裂解的聚乙二醇化：克服高效药物递送“PEG困境”的策略
DOI：
10.1080/10717544.2017.1388451
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发表时间：
2017-12
期刊：
影响因子：
6
通讯作者：
Shi K
中科院分区：
文献类型：
--
作者：
Fang Y;Xue J;Gao S;Lu A;Yang D;Jiang H;He Y;Shi K
为了延长药物的循环时间，聚乙二醇修饰通过增强药物的渗透性和滞留性（EPR）效应得到了广泛的应用，从而为更好的治疗提供了新的希望。然而，PEG化也带来了“PEG困境”，这对于药物的细胞吸收和随后的内体逃逸是困难的。因此，PEG修饰后药物的活性不可避免地丧失。为了实现有效治疗的成功药物递送，必须解决与使用PEG-脂质相关的关键问题，即“PEG困境”。本文介绍了可裂解聚乙二醇化纳米载体的发展和应用，并讨论了克服聚乙二醇困境的各种策略。与传统的载体系统相比，讨论了具有不同环境敏感性的PEG-脂质的载体系统，其可以响应于细胞内以及肿瘤微环境而实现切割。这种聪明的可切割聚乙二醇化为我们提供了一种有效的策略，以克服“PEG困境”，从而可能是一个很好的候选人，为癌症治疗的未来。
To prolong the circulation time of drug, PEGylation has been widely used via the enhanced permeability and retention (EPR) effect, thereby providing new hope for better treatment. However, PEGylation also brings the "PEG dilemma", which is difficult for the cellular absorption of drugs and subsequent endosomal escape. As a result, the activity of drugs is inevitably lost after PEG modification. To achieve successful drug delivery for effective treatment, the crucial issue associated with the use of PEG-lipids, that is, “PEG dilemma” must be addressed. In this paper, we introduced the development and application of nanocarriers with cleavable PEGylation, and discussed various strategies for overcoming the PEG dilemma. Compared to the traditional ones, the vehicle systems with different environmental-sensitive PEG-lipids were discussed, which cleavage can be achieved in response to the intracellular as well as the tumor microenvironment. This smart cleavable PEGylation provides us an efficient strategy to overcome “PEG dilemma”, thereby may be a good candidate for the cancer treatment in future.
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