维甲酸纳米颗粒混悬剂的制备及表征

Preparation and characterization of retinoic acid nanoparticle suspension

采用溶剂分散法制备了不同药物质量浓度的维甲酸纳米颗粒混悬剂 ,并对其进行了冷冻干燥 ;采用光子相关谱 (PCS)测定了冷冻干燥前后混悬剂中纳米粒子的平均粒径 ;透射电镜(TEM)观察其微观形貌 ;高效液相色谱法 (HPLC)对不同时间混悬剂中全反式维甲酸的质量浓度进行定量测定 .结果表明 ,混悬剂中维甲酸纳米粒子 (RA NP)的粒径保持在 2 0 0～ 40 0nm之间 ,大都为完整的球形 ;与维甲酸硅油 1 0～ 1 5mg/L的药物质量浓度相比 ,纳米颗粒混悬剂中有效药物的质量浓度可显著提高至 35mg/L ;药物降解速度得到明显降低 ,4周之内能维持抑制细胞增殖的有效药物质量浓度 .维甲酸纳米颗粒混悬剂有望成为一种新型的增殖性玻璃体视网膜病变 (PVR)治疗用药物载体 .

Retinoic acid (RA) nanoparticle suspensions with different concentrations were prepared by solvent-diffusion method in aqueous and freeze-drying. The mean particle sizes before and after drying were determined by photon correlation spectroscopy method and the morphology of RA nanoparticles was characterized by transmission electron microscope. The concentrations of all-trans RA (ATRA) in different time were measured by high performance liquid chromatography method to analyze drug loading and stability. The results show that the mean diameter of RA nanoparticles (RA-NP) falls into 200-400 nm. Drug loading of the system is 35 mg/L. It is demonstrated that the concentration of ATRA can be kept in the range of effective antiproliferation for 4 weeks, which indicates that RA nanoparticle suspension can effectively prolong drug release. This research demonstrates that RA nanoparticle suspension can be a potential drug carrier to prevent proliferative vitreoretinopathy (PVR).