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Materials 2015, 8(1), 216-230; doi:10.3390/ma8010216

Cholesterol-Enhanced Polylactide-Based Stereocomplex Micelle for Effective Delivery of Doxorubicin

1
Department of Urology, the First Hospital of Jilin University, Changchun 130021, China
2
Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Loo Say Chye Joachim
Received: 13 December 2014 / Accepted: 7 January 2015 / Published: 12 January 2015
(This article belongs to the Special Issue Materials for Drug Delivery)
View Full-Text   |   Download PDF [1550 KB, uploaded 12 January 2015]   |  

Abstract

Nanoscale micelles as an effective drug delivery system have attracted increasing interest in malignancy therapy. The present study reported the construction of the cholesterol-enhanced doxorubicin (DOX)-loaded poly(D-lactide)-based micelle (CDM/DOX), poly(L-lactide)-based micelle (CLM/DOX), and stereocomplex micelle (CSCM/DOX) from the equimolar enantiomeric 4-armed poly(ethylene glycol)–polylactide copolymers in aqueous condition. Compared with CDM/DOX and CLM/DOX, CSCM/DOX showed the smallest hydrodynamic size of 96 ± 4.8 nm and the slowest DOX release. The DOX-loaded micelles exhibited a weaker DOX fluorescence inside mouse renal carcinoma cells (i.e., RenCa cells) compared to free DOX·HCl, probably because of a slower DOX release. More importantly, all the DOX-loaded micelles, especially CSCM/DOX, exhibited the excellent antiproliferative efficacy that was equal to or even better than free DOX·HCl toward RenCa cells attributed to their successful internalization. Furthermore, all of the DOX-loaded micelles exhibited the satisfactory hemocompatibility compared to free DOX·HCl, indicating the great potential for systemic chemotherapy through intravenous injection. View Full-Text
Keywords: cholesterol; controlled delivery; doxorubicin; malignancy therapeutics; polylactide; stereocomplex micelle cholesterol; controlled delivery; doxorubicin; malignancy therapeutics; polylactide; stereocomplex micelle
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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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MDPI and ACS Style

Wang, J.; Xu, W.; Ding, J.; Lu, S.; Wang, X.; Wang, C.; Chen, X. Cholesterol-Enhanced Polylactide-Based Stereocomplex Micelle for Effective Delivery of Doxorubicin. Materials 2015, 8, 216-230.

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