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Improving the Carrier Stability and Drug Loading of Unimolecular Micelle-based Nanotherapeutic for Acid-actived Drug Delivery and Enhanced Antitumor Therapy

Abstract

Nanomedicine based on unimolecular micelles (UMs) has shown unique advantages of high micellar stability, programmed cargo delivery and enhanced therapeutic efficiency. Herein, we report an acid-activated amphiphilic rod-like prodrug based on a dextran (DEX) polymeric framework (DEX-PDOX-b-POEGMA, marked as DMO@DOX), which conjugates a diblock copolymer of hydrophobic doxorubicin (DOX) prodrug block and hydrophilic poly[oligo(ethylene glycol) methyl ether methacrylate] (POEGMA) block by atom transfer radical polymerization. The DMO@DOX prodrug can form nano-sized UMs in aqueous media attributed to its amphiphilic structure and achieve a very high drug loading rate of 80.4 wt %. In the presence of an acidic medium resembling tumor microenvironment, the hydrazone bond embedded in the prodrug is broken, which releases the loaded drug of DOX. The DMO@DOX prodrug shows a notable and preferential inhibition effect on the growth of tumor cells in vitro compared to healthy cells, leading to the advantageous biocompatibility and effective antitumor activity. For verification, DMO@DOX prodrug was applied in the treatment of a mouse model bearing xenograft tumors and showed remarkable therapeutic performance. This study demonstrates an effective design of UM-based nanoagents to improve the micellar stability of polymeric prodrug micelles with enhanced performance in cancer therapy.

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Publication details

The article was received on 26 May 2018, accepted on 06 Aug 2018 and first published on 08 Aug 2018


Article type: Paper
DOI: 10.1039/C8TB01384E
Citation: J. Mater. Chem. B, 2018, Accepted Manuscript
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    Improving the Carrier Stability and Drug Loading of Unimolecular Micelle-based Nanotherapeutic for Acid-actived Drug Delivery and Enhanced Antitumor Therapy

    X. Shi, S. Bai, C. Yang, X. Ma, M. Hou, J. Chen, P. Xue, C. M. Li, Y. Kang and Z. Xu, J. Mater. Chem. B, 2018, Accepted Manuscript , DOI: 10.1039/C8TB01384E

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