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首页> 外文期刊>Journal of drug targeting >Triple therapy-based targeted nanoparticles for the treatment of Helicobacter pylori.
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Triple therapy-based targeted nanoparticles for the treatment of Helicobacter pylori.

机译:基于三联疗法的靶向纳米粒子,用于治疗幽门螺杆菌。

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The main aim of drug targeting was to increase the selectivity and efficacy of drugs at the infected site and to reduce the toxicity of biotechnological entities on other parts of the body. In the present study, we selected the triple therapy (amoxicillin, clarithromycin and omeprazole) due to its synergic and additive effects, which could drastically reduce the effective dose required for the complete eradication of Helicobacter pylori and prevent the development of antibiotic resistance. The gliadin nanoparticles (GNP) vis-a-vis lectin-conjugated gliadin nanoparticles (LGNP) of triple therapy were prepared by a desolvation method and evaluated for percent entrapment efficiency, percent yield, in vitro drug release study and mucoadhesion properties of formulations. The maximum percent entrapment efficiency of formulations was in the range of 65-85%. The percent yield of formulation was about 84 +/- 2.68%. The maximum percent cumulative release of all the three drugs from formulations was in the range of 22-76%. The specificity of lectin-conjugated particles was assessed by an in vitro agglutination assay method. The developed formulation was also assessed for in vitro antibacterial study, in vivo clearance efficacy and histopathological evaluation of formulations. In the in vitro antibacterial study, the LGNP with triple therapy showed a 94.83% eradication rate that is 7.4% more than that of GNP with triple therapy (88.28%) and about 16% more than that of the plain triple therapy (P < 0.001). The targeted lectin-conjugated formulations exhibited a superior in vivo clearance efficacy when compared to the non-conjugated formulations and plain drugs.
机译:靶向药物的主要目的是提高药物在感染部位的选择性和功效,并减少生物技术实体对身体其他部位的毒性。在本研究中,由于其协同作用和累加作用,我们选择了三联疗法(阿莫西林,克拉霉素和奥美拉唑),这可能会大大降低完全根除幽门螺杆菌所需的有效剂量,并防止产生抗生素耐药性。通过去溶剂化方法制备了三联疗法的麦醇溶蛋白纳米颗粒(GNP)与凝集素结合的麦醇溶蛋白纳米颗粒(LGNP),并评价了包封率,产率,体外药物释放研究和制剂的粘膜粘附特性​​。制剂的最大包封率在65-85%的范围内。制剂的百分产率为约84 +/- 2.68%。三种药物从制剂中的最大累积释放百分比在22-76%的范围内。凝集素缀合的颗粒的特异性通过体外凝集测定法评估。还对开发的制剂进行了体外抗菌研究,体内清除效力和制剂的组织病理学评估。在体外抗菌研究中,三联疗法的LGNP根除率为94.83%,比三联疗法的GNP(88.28%)高7.4%,比普通三联疗法的根除率高16%(P <0.001 )。当与非缀合制剂和普通药物相比时,靶向凝集素缀合的制剂表现出优异的体内清除效力。

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