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双脂质体介导的双药靶向治疗幽门螺杆菌感染

Double liposomes mediated dual drug targeting for treatment of Helicobacter pylori infections.

作者信息

Singh D Yuvraj, Prasad N Kamta

机构信息

Department of Pharmaceutical Sciences, Guru Ghasidas Central University, Bilaspur, Chattisgarh, India.

出版信息

Pharmazie. 2011 May;66(5):368-73.

PMID:21699071
Abstract

In the present study the potential of phosphatidylethanolamine (PE) lipid anchored double liposomes (DL) to incorporate two drugs in a single system is exploited as a tool to augment the H. pylori eradication rate. Preparation of DL involves two steps, first formation of primary (inner) liposomes by thin film hydration method containing one drug, then addition of suspension of inner liposomes on thin film of lipid containing the other drug. The success of formation of DL was characterized by optical and transmission electron microscopy. Quantitation of DL-bacterial interaction was evaluated in terms of percent growth inhibition (%GI) on reference strain of H. pylori ATCC 26695. To confirm specific binding efficacy of DL to H. pylori PE surface receptor we performed an agglutination assay. Agglutination in DL treated H. pylori suspension suggested selectivity of DL towards the PE surface receptor of H. pylori. Monotherapy is generally not recommended for treatment of a H. pylori infection due to the danger of development of resistance and unacceptably low eradication rates. Therefore combination therapy with amoxicillin trihydrate (AMOX) as anti-H. pylori agent and ranitidine bismuth citrate (RBC) as antisecretory agent were selected for the study with an expectation that this dual-drug delivery approach will exert acceptable anti-H. pylori activity.

摘要

在本研究中,利用磷脂酰乙醇胺(PE)脂质锚定双脂质体(DL)在单一系统中包封两种药物的潜力,作为提高幽门螺杆菌根除率的一种手段。DL的制备包括两个步骤,首先通过薄膜水化法制备含有一种药物的初级(内部)脂质体,然后将内部脂质体悬浮液添加到含有另一种药物的脂质薄膜上。通过光学显微镜和透射电子显微镜对DL的形成成功进行了表征。根据对幽门螺杆菌ATCC 26695参考菌株的生长抑制百分比(%GI)评估DL与细菌相互作用的定量。为了证实DL与幽门螺杆菌PE表面受体的特异性结合效力,我们进行了凝集试验。用DL处理的幽门螺杆菌悬液中的凝集表明DL对幽门螺杆菌PE表面受体具有选择性。由于存在耐药性发展的风险和根除率低得不可接受,一般不建议采用单一疗法治疗幽门螺杆菌感染。因此,选择三水合阿莫西林(AMOX)作为抗幽门螺杆菌药物和雷尼替丁枸橼酸铋(RBC)作为抗分泌药物进行联合治疗,期望这种双药递送方法将发挥可接受的抗幽门螺杆菌活性。

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