5-氟尿嘧啶载自组装水凝胶纳米粒的制备及体外释放

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

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。

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.