中文摘要：

以中链脂肪酸甘油酯（MCT）为液态脂质，利用乳化溶剂挥发与高压均质相结合的方法制备了一种新颖的含眼膏基质的环孢素A（1）脂质纳米分散体（eyeointment—containedcyclosporineAlipidnanodispersion，1-EOCLN），用于治疗伴有炎症反应的重度干眼症。所得1-EOCLN平均粒径约90nm，多分散系数小于0．2，ζ电位低于-25mV，l的包封率高于99％。透射电镜照片显示，1-EOCLN外观形态圆整，眼膏基质均匀包裹在MCT形成的乳滴中，且主要分布于油水两相的界面。1-EOCLN的粒径与ζ电位对温度及光照敏感，4℃条件放置6个月较稳定。EOCLN保留了眼膏剂的润滑和修复泪膜功能，同时避免了眼膏剂顺应性差的不足，是～种具有临床应用前景的疏水性药物眼部递送载体。

英文摘要：

A novel eye ointment-contained cyclosporine A （1） lipid nanodispersion （1-EOCLN） for the treatment of severe dry eye syndrome accompanied with inflammation was prepared by solvent evaporation method coupled with high pressure homogenization method with medium chain triglycerides （MCT） as a liquid lipid in the formulation. The prepared 1-EOCLN had a mean particle size of about 90 nm, with a polydispersity index less than 0.2 and a ζ potential lower than -25 inV. The entrapment efficiency of 1 in EOCLN was above 99%. The image of TEM showed that 1-EOCLN had a spherical shape and the ointment matrix was evenly entrapped in the nanoemulsion of MCT, which was mostly locating at the interface between oil and aqueous phase. Particle size and ζ potential of 1-EOCLN were sensitive to higher temperature and stronger illumination. The optimized formulation was rather stable when it was stored at 4 ℃ for 6 months. The EOCLN remained the functions of eye lubrication and tear film restoration, and at the mean time avoided the poor compliance of eye ointment. For hydrophobic medicines, EOCLN could be a promising ocular delivery carrier for clinical application.