Oral Drug Delivery Systems for Ulcerative Colitis Therapy: A Comparative Study with Microparticles and Nanoparticles
Oral Drug Delivery Systems for Ulcerative Colitis Therapy: A Comparative Study with Microparticles and Nanoparticles
复制标题
用于溃疡性结肠炎治疗的口服给药系统：微粒和纳米颗粒的比较研究
DOI：
10.2174/1568009618666181016152042
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发表时间：
2019-01-01
影响因子：
3
通讯作者：
Xiao, Bo
中科院分区：
文献类型：
--
作者：
Ma, Panpan;Si, Xiaoying;Xiao, Bo
背景：口服微粒（MP）和纳米颗粒（NP）已被广泛用作治疗溃疡性结肠炎（UC）的方法。然而，之前的研究还没有比较研究MP和NP的治疗效果。方法：在本研究中，采用单一油包水乳液溶剂蒸发技术制备了负载姜黄素（CUR）的MP（CUR-MP）和负载CUR的NP（CUR-NP）。进一步比较研究了它们对UC的治疗效果。结果：所得球形MPs和NPs表现出轻微的负zeta电位，平均粒径分别约为1.7μm和270nm。结果发现，在同一调查期内，NP 的 CUR 释放率远高于 MP。体内实验表明，口服 CUR-MP 和 CUR-NP 可以减轻葡聚糖硫酸钠诱导的 UC 小鼠模型的炎症症状。重要的是，与CUR-MPs相比，CUR-NPs在缓解UC方面表现出更好的治疗效果。结论：与MPs相比，NPs可以通过增强药物释放和细胞摄取效率来提高CUR的抗炎活性。因此，它们可以被用作一种有前景的口服药物递送系统，用于有效治疗 UC。
Background: Oral administrations of microparticles (MPs) and nanoparticles (NPs) have been widely employed as therapeutic approaches for the treatment of ulcerative colitis (UC). However, no previous study has comparatively investigated the therapeutic efficacies of MPs and NPs.Methods: In this study, curcumin (CUR)-loaded MPs (CUR-MPs) and CUR-loaded NPs (CUR-NPs) were prepared using a single water-in-oil emulsion solvent evaporation technique. Their therapeutic outcomes against UC were further comparatively studied.Results: The resultant spherical MPs and NPs exhibited slightly negative zeta-potential with average particle diameters of approximately 1.7 mu m and 270 nm, respectively. It was found that NPs exhibited a much higher CUR release rate than MPs within the same period of investigation. In vivo experiments demonstrated that oral administration of CUR-MPs and CUR-NPs reduced the symptoms of inflammation in a UC mouse model induced by dextran sulfate sodium. Importantly, CUR-NPs showed much better therapeutic outcomes in alleviating UC compared with CUR-MPs.Conclusion: NPs can improve the anti-inflammatory activity of CUR by enhancing the drug release and cellular uptake efficiency, in comparison with MPs. Thus, they could be exploited as a promising oral drug delivery system for effective UC treatment.