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《Acta Pharmaceutica Sinica》 2008-01
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Recent advances in the study of cleavable PEG-lipid derivatives modifying liposomes

XU Huan,DENG Yi-hui,CHEN Da-wei(School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)  
Polyethylene glycol(PEG) lipid derivatives could increase the stability of liposomes in vivo and in vitro and prolong the circulation time of liposomes in vivo.However,the chemical bond between PEG and lipid was so stable that liposomes modified with traditional PEG-lipid derivatives could not release their contents at targeted tissue immediately and the pharmacodynamic effect was reduced.The concept of cleavable PEG-lipid was raised in recent years and these PEG-lipid derivatives could break under physiological or pathological condition.The cleavable PEG-lipid derivatives could prolong the circulation time of liposomes,and after arriving at targeted location,PEG fragment had cleaved from the surface of liposomes,so liposomes could bind with pathological cells and release contents into cells.Removal of the protective polymer layer is necessary once the liposome close to the tumour to allow to fuse and release drug.Attempts have been made to increase the circulation time and reconstitute the cellular affinity of liposomes by incorporating PEG-lipid derivatives.This review focused on the kinds of cleavable PEG-lipid derivatives,types of cleavage,the application feature to liposomes and the advantages and localizations.
【Fund】: 国家自然科学基金资助项目(30371694).
【CateGory Index】: R94
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