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Development and characterization of nanolipobeads-based dual drug delivery system for H. Pylori targeting

机译:幽门螺杆菌靶向的基于纳米脂质珠的双重药物递送系统的开发和表征

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The objective of the present investigation was to prepare and evaluate nanolipobeads which permit the targeting of drugs to H. Pylori and potentially used for the treatment of gastric ulcer. For this polyvinyl alcohol nanoparticles were prepared by freeze thaw cyclizing method and surface acylation was done by treating with (1M) palmitoyl chloride in hexane followed by addition of 0.1 N NaOH to induce acylation by adjusting pH below 6.5. Finally, nanolipobeads synthesis was carried out by combining equal parts of suspension of acylated poly vinyl alcohol nanoparticles (PVA-NPs) and AMOX encapsulated PE liposomes suspension. The uniformity of supported PE lipid layer on acylated PVA-NPs was examined using fluorescence and confocal laser scanning electron microscopy. The optimized nanolipobeads formulation demonstrated 773.3±4.3nm average age size and 84.7±2.9% of AMOX and 67.5±2.8% of RBC release up to 72h, respectively. Furthermore, binding specificity and targeting propensity toward H. pylori (SKP-56) was confirmed by agglutination and in situ adherence assay. Reduction of the absolute alcohol induced ulcerogenic index from 3.01±0.25 to 0.31±0.09 and 100% H. pylori clearance rate was observed. These results suggested that nanolipobeads are potential vector for development of dual drug delivery for effective treatment of H. pylori associated peptic ulcer.
机译:本研究的目的是制备和评估纳米脂质珠,其可将药物靶向幽门螺杆菌并潜在地用于治疗胃溃疡。对于该聚乙烯醇纳米颗粒,通过冻融环化方法制备,并且通过用(1M)棕榈酰氯的己烷溶液处理,然后添加0.1N NaOH以通过将pH值调节至6.5以下来诱导酰化,来进行表面酰化。最后,通过将等量的酰化聚乙烯醇纳米粒子(PVA-NPs)悬浮液和AMOX包封的PE脂质体悬浮液合并,进行纳米脂质珠的合成。使用荧光和共聚焦激光扫描电子显微镜检查了酰化的PVA-NPs上支持的PE脂质层的均匀性。优化的纳米脂质珠制剂在长达72h的时间里分别显示出773.3±4.3nm的平均年龄大小和84.7±2.9%的AMOX和67.5±2.8%的RBC释放。此外,通过凝集和原位粘附测定证实了对幽门螺杆菌(SKP-56)的结合特异性和靶向倾向。观察到绝对酒精诱导的致溃疡指数从3.01±0.25降低到0.31±0.09,并且幽门螺杆菌清除率降低了100%。这些结果表明,纳米脂质体是开发用于有效治疗幽门螺杆菌相关性消化性溃疡的双重药物递送的潜在载体。

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