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用于眼科药物递送的载聚合物胶束水凝胶隐形眼镜。

Polymer Micelles Laden Hydrogel Contact Lenses for Ophthalmic Drug Delivery.

作者信息

Hu Xiaohong, Tan Huaping, Chen Pin, Wang Xin, Pang Juan

出版信息

J Nanosci Nanotechnol. 2016 Jun;16(6):5480-8. doi: 10.1166/jnn.2016.11733.

Abstract

Hydrogel contact lens is an attractive drug carrier for the delivery of ophthalmic drugs. But limited drug loading capacity and burst release restricted its application in this field. Polymer micelle laden hydrogel contact lenses were designed for ophthalmic drug delivery in the work. β-CD/PAA/PEG ternary system was chosen to form polymer micelle. The micelle size could be adjusted by β-CD content and PAA/PEG concentration. The zeta potential of micelle was irrelevant to β-CD content, but influenced by PAA/PEG concentration. The absorbed drug concentration in micelle solution depended on both β-CD content and PAA/PEG concentration. Polymer micelle laden hydrogels were obtained by radical polymerization in situ. The transparency of polymer micelle laden hydrogel declined with PAA/PEG concentration increasing. The equilibrium water content and water loss showed that polymer micelle laden hydrogel with higher PAA/PEG concentration was in a higher swollen state. The dynamic viscoelastic properties howed that all polymer micelle laden hydrogels had some characteristics of crosslinked elastomers. The surface structure of freeze dried composite hydrogels was different from freeze dried pure hydrogel. The drug loading and releasing behaviors were detected to evaluate the drug loading and releasing capacity of hydrogels using orfloxacin and puerarin as model drugs. The results indicated the polymer micelle in hydrogel could hold or help to hold some ophthalmic drugs, and slow down orfloxacin release speed or keep puerarin stably stay for a time in hydrogels. In the end, it was found that the transparency of composite hydrogel became better after the hydrogel had been immersed in PBS for several weeks.

摘要

水凝胶隐形眼镜是一种用于递送眼科药物的极具吸引力的药物载体。但有限的载药量和突释现象限制了其在该领域的应用。在这项工作中,设计了负载聚合物胶束的水凝胶隐形眼镜用于眼科药物递送。选择β-环糊精/聚丙烯酸/聚乙二醇三元体系来形成聚合物胶束。胶束尺寸可通过β-环糊精含量和聚丙烯酸/聚乙二醇浓度进行调节。胶束的ζ电位与β-环糊精含量无关,但受聚丙烯酸/聚乙二醇浓度的影响。胶束溶液中药物的吸附浓度取决于β-环糊精含量和聚丙烯酸/聚乙二醇浓度。通过原位自由基聚合获得负载聚合物胶束的水凝胶。负载聚合物胶束的水凝胶的透明度随聚丙烯酸/聚乙二醇浓度的增加而降低。平衡含水量和水分损失表明,聚丙烯酸/聚乙二醇浓度较高的负载聚合物胶束的水凝胶处于较高的溶胀状态。动态粘弹性性能表明,所有负载聚合物胶束的水凝胶都具有一些交联弹性体的特性。冻干复合水凝胶的表面结构与冻干纯水性凝胶不同。以氧氟沙星和葛根素为模型药物,检测了药物的负载和释放行为,以评估水凝胶的载药和释药能力。结果表明,水凝胶中的聚合物胶束可以容纳或有助于容纳一些眼科药物,并减缓氧氟沙星的释放速度,或使葛根素在水凝胶中稳定停留一段时间。最后发现,复合水凝胶在PBS中浸泡数周后透明度变好。

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