Wu Shuangxia, Geng Fengjie, He Suqin, Liu Wentao, Liu Hao, Huang Miaoming, Zhu Chengshen
School of Materials Science and Engineering, Zhengzhou University Zhengzhou Henan 450001 PR China
Henan Key Laboratory of Advanced Nylon Materials and Application, Zhengzhou University Zhengzhou 450001 PR China.
RSC Adv. 2020 Aug 11;10(50):29668-29674. doi: 10.1039/d0ra01473g. eCollection 2020 Aug 10.
To increase the bioavailability and water solubility of hydrophobic medicine, an amphiphilic block copolymer, polycaprolactone--polyhydroxyethyl acrylamide (PCL--PHEAA), was synthesized. The copolymer can self-assemble into micelles by dialysis. The micelles were characterized by the Tyndall effect, static drop method, fluorescence spectrometry, dynamic light scattering, scanning electron microscopy and transmission electron microscopy. Ibuprofen was encapsulated inside the micelles by dialysis as a model medicine. The results show that the amphiphilic copolymer forms a uniform micelle system, with spherical micelles dispersed well in solution which have a low critical micelle concentration. In addition, the system shows good amphipathic behavior. Average particle size of a micelle is 104 nm, which increases a lot after drug loading and standing for half a month. In the first few hours, the cumulative release of the drug increases gradually; the rate of increase in the first ten hours is faster, then reaching a plateau which tends to be flat finally. It is similar under two different pH conditions. This biocompatible, biodegradable amphiphilic block copolymer has potential applications in the biomedical field.
为提高疏水性药物的生物利用度和水溶性，合成了一种两亲性嵌段共聚物聚己内酯-聚羟乙基丙烯酰胺（PCL-PHEAA）。该共聚物可通过透析自组装形成胶束。通过丁达尔效应、静滴法、荧光光谱法、动态光散射、扫描电子显微镜和透射电子显微镜对胶束进行了表征。以布洛芬作为模型药物，通过透析将其包封于胶束内部。结果表明，两亲性共聚物形成了均匀的胶束体系，球形胶束在溶液中分散良好，临界胶束浓度较低。此外，该体系表现出良好的两亲性行为。胶束的平均粒径为104nm，载药并静置半个月后粒径大幅增加。在最初几个小时内，药物的累积释放量逐渐增加；前十小时的增加速率较快，随后达到平台期并最终趋于平稳。在两种不同的pH条件下情况相似。这种具有生物相容性、可生物降解的两亲性嵌段共聚物在生物医学领域具有潜在应用价值。
