title: Intercellular pH-responsive histidine modified dextran-g-cholesterol micelle for anticancer drug delivery.
abstract: Herein, the micelles based on histidine modified dextran-g-cholesterol (HDC) were successfully prepared which exhibited excellent pH-responsive behavior in acidic aqueous solution (pH<6, within the range of malignant cellular endosome). Taking advantage of this pH-sensitivity in acidic conditions, doxorubicin (DOX), a model anticancer drug, was effectively loaded into the micelles via hydrophobic interactions. The DOX release from all DOX-loaded micelles was accelerated in acid conditions mimicking the endosomal/lysosomal compartments. The enhanced intracellular DOX release was also observed in MCF-7 cells. DOX-loaded pH-sensitive micelles showed higher cellular proliferation inhibition toward MCF-7 cells than that of pH-insensitive micelles. These features suggested that the micelles could efficiently load and deliver DOX into tumor cells, which can enhance the inhibition of cellular proliferation in vitro, providing a powerful mean for delivering and releasing cargoes at the tumor sites.
authors.affiliation: Department of Chemistry, Northeast Normal University, Changchun 130022, PR China.
authors.forename: Xuemei
authors.initials: X
authors.lastname: Yao
authors.affiliation: Department of Chemistry, Northeast Normal University, Changchun 130022, PR China. Electronic address: chenl686@nenu.edu.cn.
authors.forename: Li
authors.initials: L
authors.lastname: Chen
authors.affiliation: Department of Chemistry, Northeast Normal University, Changchun 130022, PR China.
authors.forename: Xiaofei
authors.initials: X
authors.lastname: Chen
authors.affiliation: Changchun Institutes of Applied Chemistry, Changchun 130022, PR China.
authors.forename: Chaoliang
authors.initials: C
authors.lastname: He
authors.affiliation: Changchun Institutes of Applied Chemistry, Changchun 130022, PR China.
authors.forename: Hui
authors.initials: H
authors.lastname: Zheng
authors.affiliation: Changchun Institutes of Applied Chemistry, Changchun 130022, PR China.
authors.forename: Xuesi
authors.initials: X
authors.lastname: Chen
mesh_terms: D016923:Cell Death / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D060833:Cellular Microenvironment / Q000187:drug effects; D002784:Cholesterol / Q000737:chemistry*; D003911:Dextrans / Q000737:chemistry*; D004317:Doxorubicin / Q000494:pharmacology*; D016503:Drug Delivery Systems; D005110:Extracellular Space / Q000737:chemistry*; D005434:Flow Cytometry; D006639:Histidine / Q000737:chemistry*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D061986:MCF-7 Cells; D008823:Micelles; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D066244:Proton Magnetic Resonance Spectroscopy; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D003911:Dextrans; D008823:Micelles; D011108:Polymers; D006639:Histidine; D004317:Doxorubicin; D002784:Cholesterol
keywords: Dextran-g-cholesterol; Drug delivery; Histidine; Micelle; pH-responsive