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Boronic Acid Shell‐Crosslinked Dextran‐ b‐ PLA Micelles for Acid‐Responsive Drug Delivery
Author(s) -
Zhao Ziwei,
Yao Xuemei,
Zhang Zhe,
Chen Li,
He Chaoliang,
Chen Xuesi
Publication year - 2014
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201400251
Subject(s) - micelle , chemistry , dextran , drug delivery , amphiphile , hydrolysis , boronic acid , in vitro , aqueous solution , mtt assay , in vivo , combinatorial chemistry , copolymer , biochemistry , organic chemistry , polymer , microbiology and biotechnology , biology
Herein, 3‐carboxy‐5‐nitrophenylboronic acid (CNPBA) shell‐crosslinked micelles based on amphiphilic dextran‐ block ‐polylactide (Dex‐ b ‐PLA) are prepared and used for efficient intracellular drug deliveries. Due to the reversible pH‐dependent binding with diols to form boronate esters, CNPBA modified Dex‐ b ‐PLA shows excellent pH‐sensitivity. In neutral aqueous conditions, CNPBA‐Dex‐ b ‐PLA forms shell‐crosslinked micelles to enable DOX loading, while in acid conditions, the boronate esters hydrolyze and the micelles de‐crosslink to release loaded DOX. In vitro release studies indicate that the release of the DOX cargo is minimized at physiological conditions, while there is a burst release in response to low pHs. The cell viability of CNPBA‐Dex‐ b ‐PLA investigated by MTT assay was more than 90%, indicating that, as a drug delivery system, CNPBA‐Dex‐ b ‐PLA has good cytocompatibility. These features suggest that the pH‐responsive biodegradable CNPBA‐Dex‐ b ‐PLA can efficiently load and deliver DOX into tumor cells and enhance the inhibition of cellular proliferation in vitro, providing a favorable platform as a drug delivery system for cancer therapy.