Department of Chemical Sciences, Indian Institute of Science Education and Research Kolkata, Mohanpur, West Bengal 741252, India.
Langmuir. 2011 Apr 5;27(7):3835-41. doi: 10.1021/la104461m. Epub 2011 Mar 7.
This paper presents the construction of hollow peptide microspheres and the mechanism of transition of microspheres to rod-like vesicles at low concentration. The tripeptides Boc-Phe-Maba-Phe-OMe 1 and Boc-Phe-Maba-Tyr-OMe 2, each of them containing a rigid m-aminobenzoic acid (Maba) template at the central position, forms microspheres at a concentration of 1.6 mM in methanol. At low concentration, these vesicular structures are fused through neck formation, and this leads to sphere-to-rod transition of vesicles. Sizes of these microspheres increase with increasing concentration. We have successfully characterized this transition by fluorescence spectroscopy, DLS, and electron microscopic study. The scanning electron microscopy clearly shows that these spheres are hollow. One important property of these microvesicular structures is the encapsulation of a potent anticonvulsant and mood stabilizing drug carbamazepine, which holds future promise to use these microvesicles as delivery vehicles.
本文介绍了中空肽微球的构建以及微球在低浓度下向棒状囊泡转变的机制。三肽 Boc-Phe-Maba-Phe-OMe 1 和 Boc-Phe-Maba-Tyr-OMe 2 每个分子的中心位置都含有一个刚性的间氨基苯甲酸（Maba）模板，在甲醇中的浓度为 1.6mM 时形成微球。在低浓度下，这些囊泡结构通过颈形成融合，导致囊泡的球体到棒状的转变。这些微球的尺寸随浓度的增加而增加。我们已经通过荧光光谱、DLS 和电子显微镜研究成功地对这种转变进行了表征。扫描电子显微镜清楚地显示这些球体是中空的。这些微囊泡结构的一个重要性质是封装了一种有效的抗惊厥和稳定情绪的药物卡马西平，这为使用这些微囊作为药物载体提供了未来的前景。
