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Boronic Acid Shell-Crosslinked dextran-b-PLA Micelles for Acid-Responsive Drug Delivery

Boronic Acid Shell-Crosslinked dextran-b-PLA Micelles for Acid-Responsive Drug Delivery

Ziwei Zhao, Xuemei Yao, Zhe Zhang, Li Chen, Chaoliang He, Xuesi Chen

Macromol Biosci. 2014 Nov;14(11):1609-18.

PMID: 25142134

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP101084815	3-Carboxy-5-nitrophenylboronic acid		101084-81-5	Price

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