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

Materials

Jixue Wang²  Weiguo Xu¹  Jianxun Ding¹  Shengfan Lu¹  Xiaoqing Wang²  Chunxi Wang²  Xuesi Chen¹ 

[1] Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China; E-Mails:;Department of Urology, the First Hospital of Jilin University, Changchun 130021, China; E-Mails:

关键词: cholesterol;    controlled delivery;    doxorubicin;    malignancy therapeutics;    polylactide;    stereocomplex micelle;   

DOI  :  10.3390/ma8010216

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.