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载血小板靶向脂质体递送链激酶:制备与表征。

Platelets directed liposomes for the delivery of streptokinase: development and characterization.

机构信息

Department of Pharmaceutical Sciences, Dr. H.S. Gour University, Sagar, Madhya Pradesh, India.

出版信息

Eur J Pharm Sci. 2011 Dec 18;44(5):589-94. doi: 10.1016/j.ejps.2011.10.004. Epub 2011 Oct 8.

Abstract

The present study was aimed to study the effect of RGD peptide conjugation on the bio-distribution behaviour of long circulatory liposomes in the thrombosed rat model. Further, thrombolysis study was also performed to evaluate the therapeutic activity of the prepared liposomes. Liposomes were prepared by film hydration method and peptide was subsequently conjugated on the preformed liposomes using carbodiimide chemistry. Prepared liposomes were characterized for size and size distribution, entrapment efficiency and in vitro drug release. In vitro targeting ability of the liposomes was determined by platelets binding assay. In vivo studies were performed in the rat model containing human blood clot inoculated in the carotid artery. Results of the study showed that RGD peptide conjugated liposomes significantly accumulated to the site of blood clot and higher thrombolytic activity was observed with peptide modified liposomes as compared to plain streptokinase solution and long circulatory liposomes.

摘要

本研究旨在研究 RGD 肽缀合对血栓大鼠模型中长循环脂质体的生物分布行为的影响。此外,还进行了溶栓研究,以评估所制备的脂质体的治疗活性。脂质体通过薄膜水化法制备,然后使用碳二亚胺化学将肽缀合到预形成的脂质体上。制备的脂质体进行了粒径和粒径分布、包封效率和体外药物释放的表征。通过血小板结合试验测定了脂质体的体外靶向能力。在含有接种在颈总动脉中的人血栓的大鼠模型中进行了体内研究。研究结果表明,RGD 肽修饰的脂质体显著聚集到血栓部位,与普通链激酶溶液和长循环脂质体相比,肽修饰的脂质体表现出更高的溶栓活性。

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