Oral administration of pH-sensitive curcumin-loaded microparticles for ulcerative colitis therapy.
Oral administration of pH-sensitive curcumin-loaded microparticles for ulcerative colitis therapy.
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DOI：
10.1016/j.colsurfb.2015.07.081
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发表时间：
2015-11-01
期刊：
影响因子：
--
通讯作者：
Merlin D
中科院分区：
文献类型：
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作者：
Xiao B;Si X;Zhang M;Merlin D
口服结肠特异性药物递送对于溃疡性结肠炎（UC）治疗非常有意义。在此，采用乳液-溶剂蒸发法用pH敏感的Eudragit S100（ERS100）和聚丙交酯乙交酯（PLGA）制备微粒（MP），并在MP中负载姜黄素（一种有效的抗炎剂）。所得球形 MP 的粒径范围为 1.52 至 1.91 μm。它们的装载效率可以通过改变ERS100和PLGA的重量比来调节，一些MP的装载效率超过80%。据观察，通过增加 PLGA 含量，可以显着降低缓冲液（pH 1.2 和 6.8）中 MP 中姜黄素的快速释放。重量比为 1:2 的 ERS100/PLGA MPs (MPs-4) 能够维持姜黄素的持续释放，在 20 小时的孵育过程中，在 pH 7.2-7.4 下释放约 48% 的初始载药量。最重要的是，体内实验表明，与姜黄素相比，口服 MPs-4 在缓解 UC 小鼠模型中的结肠炎方面具有优异的治疗效果。总的来说，我们的一步制备的姜黄素负载 MP 具有 pH 敏感性、受控药物释放和结肠靶向的特性，因此有望成为一种易于扩展的药物载体，用于 UC 的有效临床治疗。
Oral colon-specific drug delivery is of great interest for ulcerative colitis (UC) therapy. Here, an emulsion-solvent evaporation method was used to fabricate microparticles (MPs) with pH-sensitive Eudragit S100 (ERS100) and poly(lactide-co-glycolide) (PLGA), and the MPs were loaded with curcumin (an efficient anti-inflammatory agent). The resultant spherical MPs had a desirable particle size ranging from 1.52 to 1.91 μm. Their loading efficiency could be regulated by changing the weight ratios of ERS100 and PLGA, with some MPs exhibiting loading efficiencies over 80%. It was observed that the fast release of curcumin from MPs in buffers (pH 1.2 and 6.8) could be significantly decreased by increasing the PLGA content. ERS100/PLGA MPs with a weight ratio of 1:2 (MPs-4) were able to maintain sustained release of curcumin, releasing ~ 48% of the initial drug load at pH 7.2–7.4 during a 20 h-incubation. Most importantly, in vivo experiments revealed that orally administered MPs-4 had a superior therapeutic efficiency in alleviating colitis in a UC mouse model, compared to curcumin. Collectively, our one-stepfabricated curcumin-loaded MPs have the properties of pH-sensitivity, controlled drug release and colon targeting, and thus may hold promise as a readily scalable drug carrier for the efficient clinical treatment of UC.