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脂质体胶体系统设计用于眼部递呈环丙沙星。

Design of liposomal colloidal systems for ocular delivery of ciprofloxacin.

机构信息

College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.

Department of Pharmaceutics, College of Pharmacy, Al-Jouf University, P.O. Box 2014, Al-Jouf, Sakaka, Saudi Arabia.

出版信息

Saudi Pharm J. 2014 Jul;22(3):231-9. doi: 10.1016/j.jsps.2013.07.003. Epub 2013 Aug 8.

Abstract

Ophthalmic drug bioavailability is limited due to protective mechanisms of the eye which require the design of a system to enhance ocular delivery. In this study several liposomal formulations containing ciprofloxacin (CPX) have been formulated using reverse phase evaporation technique with final dispersion of pH 7.4. Different types of phospholipids including Phosphatidylcholine, Dipalmitoylphosphatidylcholine and Dimyristoyl-sn-glycero-3-phosphocholine were utilized. The effect of formulation factors such as type of phospholipid, cholesterol content, incorporation of positively charging inducing agents and ultrasonication on the properties of the liposomal vesicles was studied. Bioavailability of selected liposomal formulations in rabbit eye aqueous humor has been investigated and compared with that of commercially available CPX eye drops (Ciprocin®). Pharmacokinetic parameters including Cmax, Tmax, elimination rate constant, t1/2, MRT and AUC0-∞, were determined. The investigated formulations showed more than three folds of improvement in CPX ocular bioavailability compared with the commercial product.

摘要

由于眼睛的保护机制,眼科药物的生物利用度有限,这就需要设计一种系统来增强眼部递药。在这项研究中,使用反相蒸发技术制备了几种含有环丙沙星(CPX)的脂质体制剂,最终在 pH7.4 下分散。使用了包括磷脂酰胆碱、二棕榈酰磷脂酰胆碱和二肉豆蔻酰-sn-甘油-3-磷酸胆碱在内的不同类型的磷脂。研究了制剂因素(如磷脂类型、胆固醇含量、正电荷诱导剂的掺入和超声处理)对脂质体囊泡性质的影响。研究了选定的脂质体制剂在兔眼房水中的生物利用度,并与市售 CPX 眼药水(Ciprocin®)进行了比较。测定了药代动力学参数,包括 Cmax、Tmax、消除速率常数、t1/2、MRT 和 AUC0-∞。与市售产品相比,所研究的制剂使 CPX 的眼部生物利用度提高了三倍以上。

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