Glisoni Romina J, Sosnik Alejandro
The Group of Biomaterials and Nanotechnology for Improved Medicines (BIONIMED), Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires, CP1113, Argentina; National Science Research Council (CONICET), Buenos Aires, Argentina.
Macromol Biosci. 2014 Nov;14(11):1639-51. doi: 10.1002/mabi.201400235. Epub 2014 Aug 27.
In this work, we investigated for the first time the conjugation of gluconolactone to a poly(ethylene oxide)-poly(propylene oxide) block copolymer by a microwave-assisted ring opening reaction. The glucosylated copolymer was obtained with high yield (90%). A conjugation extent of approximately 100% was achieved within 15 min. The modification reduced the critical micellar concentration and increased the size of the micelles. The agglutination of the modified polymeric micelles by a soluble lectin that binds glucose confirmed the recognizability of the modified nanocarrier. Finally, the solubilization of darunavir, an anti-HIV protease inhibitor, showed a sharp increase of the aqueous solubility from 91 microgram/mL to 14.2 and 18.9 mg/mL for 10% w/v pristine and glucosylated polymeric micelles, respectively.
在这项工作中，我们首次通过微波辅助开环反应研究了葡萄糖酸内酯与聚（环氧乙烷）-聚（环氧丙烷）嵌段共聚物的共轭反应。以高产率（90%）获得了糖基化共聚物。在15分钟内实现了约100%的共轭程度。该修饰降低了临界胶束浓度并增加了胶束的尺寸。一种结合葡萄糖的可溶性凝集素对修饰的聚合物胶束的凝集证实了修饰的纳米载体的可识别性。最后，抗HIV蛋白酶抑制剂达芦那韦的增溶作用表明，对于10% w/v的原始和糖基化聚合物胶束，其水溶性分别从91微克/毫升急剧增加到14.2和18.9毫克/毫升。
