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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(eye ointment-contained cyclosporine A lipid nanodispersion,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90 nm,多分散系数小于0.2,ζ电位低于-25 mV,1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,是一种具有临床应用前景的疏水性药物眼部递送载体。
A novel liposome-containing cyclosporin A (1) lipid nanodispersion (MCT) was prepared by combining medium-chain fatty acid glyceride (MCT) eye ointment-contained cyclosporine A lipid nanodispersion, 1-EOCLN) for the treatment of severe dry eye with an inflammatory response. The average particle diameter of 1-EOCLN was about 90 nm, the polydispersity index was less than 0.2, the zeta potential was lower than -25 mV, and the entrapment efficiency of 1 was higher than 99%. TEM images showed that the appearance of 1-EOCLN was round and the ointment matrix was uniformly wrapped in the emulsion droplets formed by MCT, and mainly distributed in the interface of oil-water two-phase. The particle size and the zeta potential of 1-EOCLN are sensitive to temperature and light, and stable at 4 ℃ for 6 months. EOCLN retains the ointment lubrication and repair of tear film function, while avoiding the poor compliance ophthalmic ointment, is a promising clinical application of hydrophobic drugs eye delivery vehicle.