Stereoselective Stabilization of Polymeric Vitamin E Conjugate Micelles,Biomacromolecules

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Stereoselective Stabilization of Polymeric Vitamin E Conjugate Micelles
Biomacromolecules ( IF 5.5 ) Pub Date : 2017-11-29 00:00:00 , DOI: 10.1021/acs.biomac.7b01409
Min Gao ₁ , Jian Deng ₁ , Huiying Chu ₂ , Yu Tang ₃ , Zheng Wang _{1,

4} , Yanjun Zhao _{1,

4} , Guohui Li ₂

Affiliation

Vitamin E (α-tocopherol; TPGS) micelle is a robust nanocarrier in delivering hydrophobic active pharmaceutical ingredients, but it is suffering from poor stability that is essential in terms of pharmaceutical and biomedical applications. Taking advantage of the chirality of vitamin E, this work reports the stereoselective stabilization of polymer-vitamin E conjugate micelles. Vitamin E was covalently linked to multivalent methoxy poly(ethylene glycol)-co-poly(glutamic acid), generating amphiphilic conjugates that could self-assemble into micelles. Eight types of micelles were produced via tailored combination of polymer backbone and side chain with different chirality. The particle size and critical micelle concentration analysis demonstrated a correlation between conjugate chirality and micelle stability. The most stable micelles were obtained when poly(glutamic acid) and vitamin E both are dextrorotatory, because of the high degree of α-helix revealed by both circular dichroism spectroscopy and molecular dynamics simulation. This phenomenon was further verified by the fluorescence resonance energy transfer (FRET) analysis in HepG2 cells. The current work not only provides a method to enhance the stability of vitamin E micelles, but also adds an additional facile tool in regulating the stability of polymer conjugate micelles without changing the conjugate composition.

中文翻译：

聚合物维生素E共轭胶束的立体选择性稳定化

维生素E（α-生育酚; TPGS）胶束是递送疏水性活性药物成分的强大纳米载体，但它的稳定性较差，这在制药和生物医学应用中必不可少。利用维生素E的手性，这项工作报告了聚合物-维生素E共轭胶束的立体选择性稳定作用。维生素E被共价连接到多价甲氧基聚（乙二醇） -共-聚（谷氨酸），生成可以自组装成胶束的两亲性结合物。通过聚合物主链和具有不同手性的侧链的定制组合生产了八种类型的胶束。粒度和临界胶束浓度分析证明了共轭手性与胶束稳定性之间的相关性。当聚（谷氨酸）和维生素E都具有右旋性时，由于圆二色光谱和分子动力学模拟均显示出高α-螺旋度，因此获得了最稳定的胶束。HepG2细胞中的荧光共振能量转移（FRET）分析进一步证实了这一现象。当前的工作不仅提供了增强维生素E胶束稳定性的方法，

更新日期：2017-11-29

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