5-氟尿嘧啶载自组装水凝胶纳米粒的制备及体外释放

本实验以乙酰化普鲁兰(PA)为基质材料,采用透析法制备新型自组装水凝胶纳米粒,用以增强5-氟尿嘧啶的药物靶向性及药物选择活性,从而达到降低其毒副作用的目的。用傅立叶红外光谱仪(FT-IR)、动态光散射仪(DLS)和场发射扫描电镜(FE-SEM)对其进行表征。分别测量不同浓度、温度以及储存时间下,PA纳米粒的粒径的变化情况,以研究环境因素的改变对PA纳米粒的粒径及其粒径分布的稳定性影响。使用透析方将5-氟尿嘧啶(5-FU)物理包封于自组装纳米粒中,并模拟人体环境进行了体外释放研究。结果表明,PA纳米粒在不同环境条件下,粒径基本保持恒定,具有良好的稳定性;PA纳米粒的粒径在100nm左右,具有良好的表面球形度且分布均匀;不同环境条件变化下,粒径基本保持恒定,具有良好的稳定性;在18h内,5-FU释放量达70%左右,具有明显的缓释作用。乙酰化程度越低,5-FU的缓释效果越好,但载药量略有下降。PA纳米粒是非常具有应用前景的新型5-FU药物载体。

5- Fluorouracil- Loaded Self-Assembled Nanoparticles as a Novel Drug Carrier and in vitro Release

In order to improve the cancer-targeting and selective activity of 5-fluorocracil(5-FU),a novel drug delivery system(DDS),pullulan acetate(PA) conjugate,was synthesized by a dialysis method.5-Fu was loaded into the self-assembled nanoparticles by the same method.The drug-loaded self-assembled nanoparticles were successfully obtained and characterized in terms of particle size,morphology,drug loading efficiency and release profile.The results showed that the mean diameters of the self-assembled particles were approximately 100nm,with a uniform size distribution and good sphere morphology.The nanoparticles showed good stability at various environment conditions.The total release volume was nearly 70% within 18 hours,showing great controlled release.The nanoparticles showed better controlled release with lower pullulan acetylation degree,but the drug loading efficiency slightly decreased.The PA nanoparticles are promising for loading 5-FU in anti-cancer drug delivery system.