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Updated: Feb 10, 2026

Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Shell-Sheddable Poly(N-2-hydroxypropyl methacrylamide) Polymeric Micelles for Dual-Sensitive Release of Doxorubicin
Jiajing Zhang1, Hao Tang2, Yi Shen2
1The Key Laboratory of Geriatrics, Beijing Hospital and Beijing Institute of Geriatrics, Chinese Ministry of Health, Beijing, 100730, China.
Abstract:
Poly(ethylene glycol) (PEG) shell-sheddable micelles are proved to be effective tools for rapid intracellular drug delivery. However, some adverse factors, such as the potential immunogenicity and the accelerated blood clearance, might be accompanied with the traditional PEG sheddable micelles. Here, a poly(N-2-hydroxypropyl methacrylamide) (PHPMA) sheddable block copolymer containing disulfide bonds on the main chain is prepared to form pH- and reduction-dual-responsive micelles. The most optimal synthetic route of the block copolymer is selected from three potential pathways. Doxorubicin is loaded via an acid-labile hydrazone bond to achieve high drug loading content and to prevent premature drug release. As expected, as-prepared shell-sheddable micelles exhibit faster intracellular drug release and more satisfactory in vitro anticancer efficacy than the nonsheddable counterpart did. This design provides a feasible guideline for the efficient synthesis of similar shell-sheddable micelles consisting of PHPMA coatings.
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