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Preparation and characterization of pH-sensitive nanoparticles of budesonide for the treatment of ulcerative colitis

机译:用于治疗溃疡性结肠炎的布地奈德pH敏感纳米颗粒的制备和表征

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Objective: The aim of this study was to develop pH sensitive nanoparticles of budesonide for the treatment of ulcerative colitis. Methods: The NPs system was characterized by the transmission electron microscopy (TEM), particle size, drug loading and encapsulation efficiency. In addition, in vitro drug release properties and pharmacokinetics were also investigated in detail. The optimized formulation was examined for its in-vivo targeting potential using 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced colitis in a rat model. Results: Dynamic light-scattering results showed that the particle size of budesonide-Eudragit S100/poly(lactic-co-glycolic acid) nanoparticles was around 110.5 nm, with a polydispersity index of 0.098. Transmission electron microscopy images showed that BUD-ES100/PLGA NPs were spherical with uniform size and relatively smooth surfaces. In vitro release showed that BUD-ES100/PLGA NPs required minimal release of drugs during its transit in the stomach and the upper small intestine to ensure that a maximum dose reached the colon. After the pharmacodynamic treatment, the myeloperoxidase value of BUD-ES100/PLGA NPs was close to the normal group. The histopathological examination of rectum showed that no sign of damages such as epithelial necrosis and sloughing epithelial cells was detected. Conclusion: Our findings suggested that BUD-ES100/PLGA NPs were a promising alternative to single pH-dependent systems for colitis therapy.
机译:目的:本研究的目的是开发布地奈德对pH敏感的纳米颗粒,用于治疗溃疡性结肠炎。方法:采用透射电镜(TEM),粒径,载药量和包封率对NPs体系进行表征。另外,还详细研究了体外药物释放特性和药代动力学。在大鼠模型中,使用2,4,6-三硝基苯磺酸(TNBS)诱导的结肠炎检查了优化的制剂的体内靶向潜力。结果:动态光散射结果表明,布地奈德-Eudragit S100 /聚乳酸-乙醇酸共聚物纳米粒子的粒径约为110.5 nm,多分散指数为0.098。透射电子显微镜图像显示,BUD-ES100 / PLGA NP为球形,尺寸均匀,表面相对光滑。体外释放表明,BUD-ES100 / PLGA NP在胃和上部小肠运输过程中需要药物的最小释放,以确保最大剂量到达结肠。药物动力学处理后,BUD-ES100 / PLGA NPs的髓过氧化物酶值接近正常组。直肠的组织病理学检查未发现损伤迹象,如上皮坏死和上皮细胞脱落。结论:我们的发现表明,BUD-ES100 / PLGA NP是用于结肠炎治疗的单一pH依赖系统的有前途的替代方案。

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