a Department of Pharmaceutics , School of Pharmaceutical Science, Shenyang Pharmaceutical University , Shenyang , China.
Drug Deliv. 2017 Dec;24(sup1):22-32. doi: 10.1080/10717544.2017.1388451.
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.
为了延长药物的循环时间，通过增强通透性和保留（EPR）效应，已广泛使用聚乙二醇化（PEGylation），从而为更好的治疗提供了新的希望。然而，PEGylation 也带来了“PEG 困境”，即药物难以被细胞吸收，随后无法从内体中逃逸。因此，PEG 修饰后药物的活性不可避免地会丢失。为了实现有效的治疗性药物输送，使用聚乙二醇化脂质时必须解决与关键问题相关的问题，即“PEG 困境”。本文介绍了具有可切割聚乙二醇化的纳米载体的开发和应用，并讨论了克服 PEG 困境的各种策略。与传统的脂质体相比，讨论了具有不同环境敏感型聚乙二醇化脂质的载体系统，其可以在细胞内以及肿瘤微环境中响应发生切割。这种智能可切割聚乙二醇化提供了克服“PEG 困境”的有效策略，因此可能是未来癌症治疗的良好候选者。
Zotero 插件
