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罗氟沙星负载罗望子胶多糖纳米颗粒在三硝基苯磺酸诱导的Wistar大鼠炎症性肠病模型中的治疗效果

Therapeutic efficacy of rifaximin loaded tamarind gum polysaccharide nanoparticles in TNBS induced IBD model Wistar rats.

作者信息

Amaldoss Maria John Newton, Najar Imtiyaz Ahmed, Kumar Jatinder, Sharma Archana

机构信息

Australian Centre for Nanomedicine, University of New South Wales, Sydney, NSW 2052, Australia.

Lowy Cancer Research Centre, Prince of Wales Clinical School, University of New South Wales, Sydney, NSW 2052, Australia.

出版信息

Rep Pract Oncol Radiother. 2021 Sep 30;26(5):712-729. doi: 10.5603/RPOR.a2021.0100. eCollection 2021.

Abstract

BACKGROUND

Rifaximin is a non-systemic antibiotic used in the treatment of inflammatory bowel disease (IBD). Antibiotics are demonstrating a significant role in the treatment of IBD by altering the dysbiotic colonic microbiota and decreases the immunogenic and inflammatory response in the patient population. Mucoadhesive colon targeted nanoparticles provide the site-specific delivery and extended stay in the colon. Since the bacteria occupy the lumen, spread over the surface of epithelial cells, and adhere to the mucosa, delivering the rifaximin as a nanoparticles with the mucoadhesive polymer enhances the therapeutic efficacy in IBD. The objective was to fabricate and characterize the rifaximin loaded tamarind gum nanoparticles and study the therapeutic efficacy in the TNBS-induced IBD model rats.

MATERIALS AND METHODS

The experimentation includes fabrication and characterization of drug excipient compatibility by FTIR. The fabricated nanoparticles were characterized for the hydrodynamic size and zeta potential by photon correlation spectroscopy and also analyzed by TEM. Selected best formulation was subjected to the therapeutic efficacy study in TNBS-induced IBD rats, and the macroscopic, microscopic and biochemical parameters were reported.

RESULTS

The study demonstrated that the formulation TGN1 is best formulation in terms of nanoparticle characterization and hydrodynamic size which showed the hydrodynamic size of 171.4 nm and the zeta potential of -26.44 mV and other parameters such as TEM and drug release studies were also reported.

CONCLUSIONS

The therapeutic efficacy study revealed that TGN1 is efficiently reduced the IBD inflammatory conditions as compared to the TNBS control group and reference drug mesalamine group.

摘要

背景

利福昔明是一种用于治疗炎症性肠病(IBD)的非全身性抗生素。抗生素通过改变结肠微生物群落失调,在IBD治疗中发挥着重要作用,并降低患者群体中的免疫原性和炎症反应。黏膜黏附性结肠靶向纳米颗粒可实现药物在结肠的靶向递送和延长停留时间。由于细菌占据肠腔、扩散至上皮细胞表面并黏附于黏膜,将利福昔明制成含有黏膜黏附性聚合物的纳米颗粒可提高IBD的治疗效果。目的是制备并表征负载利福昔明的罗望子胶纳米颗粒,并研究其在三硝基苯磺酸(TNBS)诱导的IBD模型大鼠中的治疗效果。

材料与方法

实验包括通过傅里叶变换红外光谱(FTIR)对药物辅料相容性进行制备和表征。通过光子相关光谱法对制备的纳米颗粒的流体动力学尺寸和zeta电位进行表征,并通过透射电子显微镜(TEM)进行分析。选择最佳制剂在TNBS诱导的IBD大鼠中进行治疗效果研究,并报告宏观、微观和生化参数。

结果

研究表明,就纳米颗粒表征和流体动力学尺寸而言,制剂TGN1是最佳制剂,其流体动力学尺寸为171.4 nm,zeta电位为-26.44 mV,还报告了其他参数,如TEM和药物释放研究结果。

结论

治疗效果研究表明,与TNBS对照组和参比药物美沙拉嗪组相比,TGN1能有效减轻IBD的炎症状况。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e43/8575354/04eb1f29e869/rpor-26-5-712f1.jpg

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