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Int. J. Mol. Sci. 2018, 19(6), 1615;

Preparation and Characterization of Electrostatically Crosslinked Polymer–Liposomes in Anticancer Therapy

School of Pharmacy, China Medical University, Taichung City 402, Taiwan
Department of Biomedical Engineering, National Yang Ming University, Taipei City 112, Taiwan
Author to whom correspondence should be addressed.
Received: 1 May 2018 / Revised: 27 May 2018 / Accepted: 28 May 2018 / Published: 30 May 2018
(This article belongs to the Special Issue Nanotechnology in Drug Delivery)
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pH-sensitive polymer–liposomes can rapidly release their payloads. However, it is difficult to simultaneously achieve stability and pH-responsiveness in the polymer–liposomes. In this study, stable and pH-sensitive crosslinked polymer–liposomes were fabricated through electrostatic interactions. The pH-sensitive copolymer methoxy poly(ethylene glycol)-block-poly(methacrylic acid)-cholesterol (mPEG-b-P(MAAc)-chol) and crosslinking reagent poly(ethylene glycol) with end-capped with lysine (PEG-Lys2) were synthesized and characterized. At physiological conditions, the pH-sensitive copolymers were anionic and interacted electrostatically with the cationic crosslinker PEG-Lys2, forming the electrostatically-crosslinked polymer–liposomes and stabilizing the liposomal structure. At pH 5.0, the carboxylic groups in mPEG-b-P(MAAc)-chol were neutralized, and the liposomal structure was destroyed. The particle size of the crosslinked polymer–liposomes was approximately 140 nm and the polymer–liposomes were loaded with the anticancer drug doxorubicin. At pH 7.4, the crosslinked polymer–liposomes exhibited good stability with steady particle size and low drug leakage, even in the presence of fetal bovine serum. At pH 5.0, the architecture of the crosslinked polymer–liposomes was damaged following rapid drug release, as observed by using transmission electron microscopy and their apparent size variation. The crosslinked polymer–liposomes were pH-sensitive within the endosome and in the human breast cancer cells MDA-MB-231, as determined by using confocal laser scanning microscopy. The intracellular drug release profiles indicated cytotoxicity in cancer cells. These results indicated that the highly-stable and pH-sensitive electrostatically-crosslinked polymer–liposomes offered a potent drug-delivery system for use in anticancer therapies. View Full-Text
Keywords: liposome; anticancer therapy; pH-sensitivity; polymer liposome; anticancer therapy; pH-sensitivity; polymer

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Chiang, Y.-T.; Lyu, S.-Y.; Wen, Y.-H.; Lo, C.-L. Preparation and Characterization of Electrostatically Crosslinked Polymer–Liposomes in Anticancer Therapy. Int. J. Mol. Sci. 2018, 19, 1615.

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