pH-triggered reversible "stealth" polycationic micelles
Gu, Jingxia1; Cheng, Woei-Ping2; Liu, Jiguang1; Lo, Sum-Yee2; Smith, David2; Qu, Xiaozhong1; Yang, Zhenzhong1
AbstractAmphiphilic polycations with a "stealth" cationic nature have been designed and synthesized by the PEGylation of polycationic amphiphile via a novel pH responsible benzoic imine linker. The linkage is stable in aqueous solution at physiological pH but cleaves in slight acidic conditions such as the extracellular environment of solid tumor and endosomes. The polymeric micelle formed from the amphiphilic "stealth" polycation contains a pH-switchable cationic surface driven by the reversible detachment/reattachment of the shielding PEG chains due to the cleavage/formation process of the imine linkage. At physiological pH, the micellar surface was shielded by the PEG corona, leading to lower cytotoxicity and less hemolysis, whereas in a mild acidic condition like in endosomes or solid tumors, the deshielding of the PEG chains exposed the positive charge on the micellar surface and retained the membrane disrupting ability. The amphiphilic "stealth" polycation is potentially useful as a drug targeting system toward tumors via endocytosis and trafficked through the endosomal pathway.
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WOS IDWOS:000252415600035
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Cited Times:140[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Corresponding AuthorQu, Xiaozhong
Affiliation1.Chinese Acad Sci, Inst Chem, State Key Lan Polymer Phys & Chem, Beijing 100080, Peoples R China
2.Robert Gordon Univ, Sch Pharm, Aberdeen AB10 1FR, Scotland
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GB/T 7714
Gu, Jingxia,Cheng, Woei-Ping,Liu, Jiguang,et al. pH-triggered reversible "stealth" polycationic micelles[J]. BIOMACROMOLECULES,2008,9(1):255-262.
APA Gu, Jingxia.,Cheng, Woei-Ping.,Liu, Jiguang.,Lo, Sum-Yee.,Smith, David.,...&Yang, Zhenzhong.(2008).pH-triggered reversible "stealth" polycationic micelles.BIOMACROMOLECULES,9(1),255-262.
MLA Gu, Jingxia,et al."pH-triggered reversible "stealth" polycationic micelles".BIOMACROMOLECULES 9.1(2008):255-262.
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