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Stereocomplex-Reinforced PEGylated Polylactide Micelle for Optimized Drug Delivery

Department of Anesthesiology, The First Hospital of Jilin University, Changchun 130021, China
Department of Chemistry, Northeast Normal University, Changchun 130024, China
Authors to whom correspondence should be addressed.
Academic Editor: Jianxun Ding
Polymers 2016, 8(4), 165;
Received: 28 March 2016 / Revised: 19 April 2016 / Accepted: 20 April 2016 / Published: 22 April 2016
(This article belongs to the Special Issue Functional Polymers for Medical Applications)
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The instability of PEGylated polylactide micelles is a challenge for drug delivery. Stereocomplex interaction between racemic polylactide chains with different configurations provides an effective strategy to enhance the stability of micelles as the nanocarriers of drugs. In this work, a stereocomplex micelle (SCM) self-assembled from the amphiphilic triblock copolymers comprising poly(ethylene glycol) (PEG), and dextrorotatory and levorotatory polylactides (PDLA and PLLA) was applied for efficient drug delivery. The spherical SCM showed the smallest scale and the lowest critical micelle concentration (CMC) than the micelles with single components attributed to the stereocomplex interaction between PDLA and PLLA. 10-Hydroxycamptothecin (HCPT) as a model antitumor drug was loaded into micelles. Compared with the loading micelles from individual PDLA and PLLA, the HCPT-loaded SCM exhibited the highest drug loading efficiency (DLE) and the slowest drug release in phosphate-buffered saline (PBS) at pH 7.4, indicating its enhanced stability in circulation. More fascinatingly, the laden SCM was demonstrated to have the highest cellular uptake of HCPT and suppress malignant cells most effectively in comparison to the HCPT-loaded micelles from single copolymer. In summary, the stereocomplex-enhanced PLA–PEG–PLA micelle may be promising for optimized drug delivery in the clinic. View Full-Text
Keywords: controlled drug delivery; malignancy therapy; polylactide; self-assembly; stereocomplex interaction controlled drug delivery; malignancy therapy; polylactide; self-assembly; stereocomplex interaction

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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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Feng, C.; Piao, M.; Li, D. Stereocomplex-Reinforced PEGylated Polylactide Micelle for Optimized Drug Delivery. Polymers 2016, 8, 165.

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