Preparationan And Basic Research On Prevention Of Proliferative Vitreoretinopathy Of Tetrandrine And 5-fluorouracil Polylactic Acid Microspheres

In the article, tetrandrine(TET) and 5-fluorouracil(5-Fu) microspheres (MS) were prepared by improved emulsify-solvent evaporation method with polylactic acid (PLA) being used as carriermaterials. On the basis of single factor investigation, use the orthogonal experiment to optimize the best prescription in order to gain the best technics and prescription for preparing microspheres. And then study the shape characteristics, the release features in vitro, the preliminary stability, the histocompatibility, the toxicity and pharmacodynamics in vivo of mice.The TET and 5-Fu-PLA-MS prepared according to the optimized technics and prescription have good dispersity and fluidity. Observed by EPMA, the ballability of it is good, the appearance is rounded and the surface is smooth. Observed by SEM, the surface of spherical particles have pores. The size distribution of microspheres is narrow. The average particle size was about 63.4μn with 89.5% of the microspheres being in the range of 50～80μm. The average drug loading and encapsulation efficiency of 5-Fu were (6.37±0.189)%, (57.30±1.687)%respectively, and that of TET were (2.54±0.115)%, (46.29±1.089)%. respectively. In vitro release of 5-Fu and TET from microspheres could be described by Higuchi model and had a good sustained release characteristic. the preliminary stability test indicate that the chemical stability of The TET and 5-Fu-PLA-MS is good.60Co radiation has no effect on the surface morphology and the content of 5-Fu and TET. Experiments in mice showed that the histocompatibility of TET and 5-Fu-PLA-MS is good.The microspheres administered into vitreous cavity of rabbits could prevent and treat experimental traumatic proliferative vitreoretinopathy safely and effectively.