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目的探讨由维甲酸和海藻酸钠制成海藻酸钠-维甲酸(AGS-RA)微球药物缓释系统的动物体内外药物释放特点。方法有机溶剂将维甲酸溶解,与1.5%的海藻酸钠均匀混合,用静电微囊发生器一次成型制作海藻酸盐-维甲酸微球;镜下观察测量微球的形态和大小,并用紫外分光光度仪测定微球的药物含量;体外释药实验则通过紫外分光光度仪和高压液相的方法测定 RA 的体外释放规律;体内实验则是通过玻璃体腔注入 AGS-RA 药物微球,利用高压液相的方法观察微球的房水药代动力学特点。结果 AGS-RA 微球经测定,大小是(95.2443±8.6265)μm;药物包含量是(1.7644±0.0453)μg/mg;体外实验表明 AGS-RA 微球的 RA 药物在观察的28d 内均匀释放;房水药代动力学研究显示药物在6周内基本均匀释放[1、3d,1、2、3、4、5、6周房水 RA 浓度分别是(23.79±0.15)、(33.45±0.48)、(19.95±0.79)、(21.12±0.47)、(19.65±0.35)、(20.01±0.25)、(18.24±0.27)、(18.5±0.68)ng/ml],仅第3天有1个释放峰。结论兔体内外实验表明,AGS-RA 微球可对药物RA 起缓释作用。
OBJECTIVE: To investigate the drug release characteristics of AGS-RA microspheres in vitro and in vivo by retinoic acid and sodium alginate. Methods Alginate was dissolved in organic solvent and uniformly mixed with sodium alginate (1.5%). Alginate-retinoic acid microspheres were fabricated by electrostatic microcapsule molding. Morphology and size of the microspheres were observed microscopically and analyzed by ultraviolet spectroscopy Spectrophotometer was used to determine the drug content of microspheres. In vitro drug release assay was used to determine the in vitro release of RA by ultraviolet spectrophotometer and high pressure liquid phase. AGS-RA drug microspheres were injected into vitreous cavity in vivo. Phase method to observe the microsphere aqueous humor pharmacokinetic characteristics. Results AGS-RA microspheres were (95.2443 ± 8.6265) μm in size and (1.7644 ± 0.0453) μg / mg in diameter. The in vitro experiments showed that the RA drug of AGS-RA microspheres was uniformly released within 28 days of observation. Pharmacokinetics of aqueous humor showed that the drug release was basically uniform within 6 weeks [(1,3,7,9 ± 0.15), (33.45 ± 0.48) and , (19.95 ± 0.79), (21.12 ± 0.47), (19.65 ± 0.35), (20.01 ± 0.25), (18.24 ± 0.27), (18.5 ± 0.68) ng / ml] . Conclusion In vitro and in vivo experiments in rabbits show that AGS-RA microspheres can release drug RA slowly.