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改良烧伤疗法:莫匹罗星脂质体-水凝胶递药系统。

Improved burns therapy: liposomes-in-hydrogel delivery system for mupirocin.

机构信息

Drug Transport and Delivery Research Group, Department of Pharmacy, Faculty of Health Sciences, University of Tromsø, Tromsø N-9037, Norway.

出版信息

J Pharm Sci. 2012 Oct;101(10):3906-15. doi: 10.1002/jps.23260. Epub 2012 Jul 9.

Abstract

Wounds, particularly burns, are prone to colonization of potentially life-threatening bacteria. Local delivery of antimicrobial agents in sufficient quantities and over longer period of time can reduce risk of burn infections. Mupirocin-in-liposomes-in-hydrogels were proposed as advanced delivery system for improved burn therapy. Mupirocin was entrapped in phosphatidylcholine liposomes of various sizes, namely larger (micron size) vesicles entrapping 74% of drug and sonicated vesicles (below 300 nm) entrapping 49% of drug. Liposomes containing mupirocin were incorporated in chitosan hydrogels (10%, w/w). Incorporation of liposomes in hydrogels resulted in prolonged release of liposomally associated mupirocin, as observed in both in vitro and ex vivo studies. The drug release was affected by the vesicle size. Microbiological evaluation of newly developed system confirmed its antimicrobial potential against Staphylococcus aureus and Bacillus subtilis. Bioadhesiveness of the system was compared with the marketed cream containing mupirocin. Our system exhibited superior bioadhesiveness and sustained mupirocin release profiles to marketed product.

摘要

创伤,特别是烧伤,容易被潜在危及生命的细菌定植。局部给予足够数量和更长时间的抗菌药物可以降低烧伤感染的风险。载抗生素脂质体-水凝胶被提议作为一种先进的给药系统,以改善烧伤治疗。莫匹罗星被包裹在不同大小的磷脂酰胆碱脂质体中,即较大(微米大小)的囊泡包裹 74%的药物,而超声处理的囊泡(小于 300nm)则包裹 49%的药物。载有莫匹罗星的脂质体被掺入壳聚糖水凝胶(10%,w/w)中。在体外和体内研究中都观察到,脂质体在水凝胶中的掺入导致与脂质体相关的莫匹罗星的释放延长。药物释放受到囊泡大小的影响。对新开发系统的微生物学评估证实了其对金黄色葡萄球菌和枯草芽孢杆菌的抗菌潜力。与市售的含莫匹罗星乳膏相比,对该系统的生物黏附性进行了比较。我们的系统表现出优于市售产品的优越的生物黏附性和持续的莫匹罗星释放曲线。

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