利福昔明-壳聚糖纳米颗粒治疗炎性肠病(IBD)。

IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics
J. Kumar, A. Newton
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引用次数: 19

摘要

背景炎症性肠病(IBD)不易控制,复发对医生来说是最具挑战性的问题。有各种可控和结肠靶向药物递送系统可用于治疗,但成功率有限。使用结肠靶向聚合物(如壳聚糖)制备的纳米粒子由于其较小的尺寸、独特的物理化学性质和靶向潜力,可以改善IBD。目的利用线性多糖壳聚糖制备利福昔明结肠靶向多糖纳米颗粒(RFX),以提高利福昔敏的溶解度、整体疗效和结肠靶向性。方法采用离子凝胶法研制用于治疗炎症性肠病(IBD)的RFX纳米粒子。通过Master Sizer和Zeta Sizer对纳米颗粒进行了各种表征技术,如XRD、FTIR和平均粒径(MPS)。还测定了所开发制剂的透射电子显微镜(TEM)、药物包封效率和ζ电位。在模拟胃、肠和结肠pH条件的缓冲条件下,使用透析袋扩散技术在体外研究了制剂的药物释放效率。结果所制备的纳米颗粒的尺寸在纳米范围内。药物释放曲线在上消化道中得到控制,并且在结肠条件下释放最大量的药物。制备的纳米颗粒显著提高了利福昔明的溶解度。最佳壳聚糖制剂的ζ电位为37.79,这证实了所制备的纳米悬浮液的稳定性。结论小颗粒纳米颗粒具有较高的包封效率和相对较高的负载能力,并具有预定的体外释放特性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Rifaximin - Chitosan Nanoparticles for Inflammatory Bowel Disease (IBD).
BACKGROUND Inflammatory Bowel Disease (IBD) cannot be controlled easily and the recurrence is the most challenging issue for the physicians. There are various controlled and colon targeted drug delivery systems available for the treatment with limited success rate. Nanoparticles prepared by using the colon targeted polymers such as chitosan may improve the IBD due to their smaller size, unique physico chemical properties and targeting potential. OBJECTIVE The aim of this investigation was designed to formulate and develop a colon targeted polysaccharide nanoparticles of rifaximin (RFX) by using linear polysaccharide chitosan, for the improvement of rifaximin solubility, overall therapeutic efficacy and colon targeting. METHODS The research was focused on developing RFX nanoparticles for the treatment of Inflammatory Bowel Disease (IBD) by ionic gelation method. Nanoparticles were subjected to various characterization techniques such as XRD, FTIR and mean particle size (MPS) by Master Sizer and Zeta Sizer. Transmission Electron Microscopy (TEM), drug entrapment efficiency and zeta potential are also determined for the developed formulations. The efficiency of drug release from prepared formulation was studied in vitro by using a dialysis bag diffusion technique in the buffer condition mimicking stomach, intestine and colonic pH conditions. RESULTS The prepared nanoparticles demonstrated the size in the nano range. The drug release profile was controlled in the upper GI tract and the maximum amount of drug was released in the colonic conditions. The prepared nanoparticles significantly improved the solubility of rifaximin. The zeta potential of the best chitosan preparation was found to be 37.79, which confirms the stability of prepared nanosuspension. CONCLUSION Nanoparticles with small particle size found to have high encapsulation efficiency and relatively high loading capacity and predetermined in vitro release profile.
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来源期刊
CiteScore
3.90
自引率
0.00%
发文量
0
期刊介绍: Recent Patents on Inflammation & Allergy Drug Discovery publishes review articles by experts on recent patents in the field of inflammation and allergy drug discovery e.g. on novel bioactive compounds, analogs and targets. A selection of important and recent patents in the field is also included in the journal. The journal is essential reading for all researchers involved in inflammation and allergy drug design and discovery.
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