ICCAS OpenIR
Preparation of Multifunctional Drug Carrier for Tumor-Specific Uptake and Enhanced Intracellular Delivery through the Conjugation of Weak Acid Labile Linker
Ding, Caixia; Gu, Jingxia; Qu, Xiaozhong; Yang, Zhenzhong
2009-06-01
Source PublicationBIOCONJUGATE CHEMISTRY
ISSN1043-1802
Volume20Issue:6Pages:1163-1170
AbstractWe demonstrate that multifuctional drug carriers, e.g., polymeric micelles, for tumor-specific uptake and intracellular delivery can be generated from the pH-dependent progressive hydrolysis of a novel benzoic-imine linker in the micelle-forming amphiphilic polymer. The linker, hence the micelle, is stable at physiological pH, partially hydrolyzes at the extracellular pH of the solid tumor, and completely hydrolyzes at the endosomal pH. Meanwhile, the surface property of the micelle converts from neutral to positively charged due to the generation of amino groups from the cleavage of the imine bond at tumor pH. The ionization on the surface facilitates the cellular uptake of the micelles through the electrostatic interaction between the micelle and the cell membrane. Subsequently, at the endosomal pH, with more complete cleavage of the polymer the micellar structure dissociates, and the system becomes very membrane-disruptive, inferring an enhanced intracellular delivery capability via the endosomal pathway.
DOI10.1021/bc800563g
Indexed BySCI
Language英语
WOS IDWOS:000267117600010
PublisherAMER CHEMICAL SOC
Citation statistics
Cited Times:128[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.iccas.ac.cn/handle/121111/66610
Collection中国科学院化学研究所
Corresponding AuthorQu, Xiaozhong
AffiliationChinese Acad Sci, Inst Chem, State Key Lab Polymer Phys & Chem, Beijing 100190, Peoples R China
Recommended Citation
GB/T 7714
Ding, Caixia,Gu, Jingxia,Qu, Xiaozhong,et al. Preparation of Multifunctional Drug Carrier for Tumor-Specific Uptake and Enhanced Intracellular Delivery through the Conjugation of Weak Acid Labile Linker[J]. BIOCONJUGATE CHEMISTRY,2009,20(6):1163-1170.
APA Ding, Caixia,Gu, Jingxia,Qu, Xiaozhong,&Yang, Zhenzhong.(2009).Preparation of Multifunctional Drug Carrier for Tumor-Specific Uptake and Enhanced Intracellular Delivery through the Conjugation of Weak Acid Labile Linker.BIOCONJUGATE CHEMISTRY,20(6),1163-1170.
MLA Ding, Caixia,et al."Preparation of Multifunctional Drug Carrier for Tumor-Specific Uptake and Enhanced Intracellular Delivery through the Conjugation of Weak Acid Labile Linker".BIOCONJUGATE CHEMISTRY 20.6(2009):1163-1170.
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