Lavasanifar A, Samuel J, Kwon G S
Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta T6G 2N8, Canada.
J Biomed Mater Res. 2000 Dec 15;52(4):831-5. doi: 10.1002/1097-4636(20001215)52:4<831::aid-jbm29>3.0.co;2-k.
Stearic acid esters of poly(ethylene oxide)-block-poly(hydroxyethyl L-aspartamide) and poly(ethylene oxide)-block-poly(hydroxyhexyl L-aspartamide) have been synthesized from poly(ethylene oxide)-block-poly(beta-benzyl L-aspartate) by polymer-analogous reactions and self-assembled into a micelle. Transmission electron microscopy and fluorescent probe studies reveal that the micelle mimics structural features of serum lipoproteins: it is nanoscopic, spherical, and has a supramolecular core-shell architecture, where the core is rich in fatty acid esters. As a result, the polymeric micelles effectively solubilize amphotericin B, a key drug for systemic mycoses. Serum lipoproteins solubilize many hydrophobic drugs as a biological transport system besides amphotericin B. A synthetic polymeric analogue may achieve the same aim, but with the ease of structural modification, safety, and stability.
通过聚合物类似反应，由聚（环氧乙烷）-嵌段-聚（β-苄基-L-天冬氨酸酯）合成了聚（环氧乙烷）-嵌段-聚（羟乙基-L-天冬酰胺）和聚（环氧乙烷）-嵌段-聚（羟己基-L-天冬酰胺）的硬脂酸酯，并自组装成胶束。透射电子显微镜和荧光探针研究表明，该胶束模拟了血清脂蛋白的结构特征：它是纳米级的、球形的，具有超分子核壳结构，其中核富含脂肪酸酯。因此，该聚合物胶束能有效增溶两性霉素B，这是一种治疗全身性真菌病的关键药物。除两性霉素B外，血清脂蛋白作为一种生物转运系统还能增溶许多疏水性药物。一种合成聚合物类似物可能实现相同的目标，但具有结构修饰容易、安全性和稳定性好的特点。
