目的:制备以PLGA和2-HP-β-CD为载体的曲安奈德(TA)滴眼液,并对其体系进行表征。方法:采用乳化溶剂挥发法制备TA-PLGA-2-HP-β-CD滴眼液,通过差示扫描、傅立叶红外、X-射线粉末衍射等方法对其理化性质进行表征,并对体外转运特性进行探讨。结果:所制备滴眼液中的纳米粒粒径为(161.7±45.5)nm,ζ-(-6.27±0.12)mV,包封率为(76.39±4.84)%,体外6 h单位面积累积释放度为40%。结论:TA-PLGA-2-HP-β-CD滴眼液体外释放规律符合零级动力学方程,其体外转运特性可为滴眼液的细胞动力学过程的选择和设计提供定量描述的基础。
OBJECTIVE To characterize and evaluate in vitro transportation characteristics of triamcinolone acetonide eyedrops with PLGA and 2-HP-β-CD as carriers.METHODS TA-PLGA-2-HP-β-CD eyedrops were prepared by modified emulsion solvent evaporation method. Then in vitro evaluations were conducted by tests of entrapment efficiency, accumulative release, morphous investigation, DSC, FT-IR and X-ray powder.RESULTS Mean entrapment efficiency of triamcinolone acetonide loaded nanocarriers was (76.39±4.84)%. Average size was (161.7±45.5)nm and in vitro cumulative release of triamcinolone acetonide from nanocarriers was 40% in 6 h.CONCLUSION Release in vitro of TA-PLGA-2-HP-β-CD eyedrops is accordant with zero order model. Intracellular kinetics can provide some information on rational choices and design of nanoparticles drug delivery system.