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本研究将具有肝靶向性分子甘草次酸(GA)偶联在具有生物相容性和生物可降解性的天然高分子海藻酸钠(ALG)上,合成了甘草次酸改性的海藻酸钠(GA-ALG);对广谱抗癌药物阿霉素(DOX)进行包封,制备了肝靶向载药纳米粒,并考察了GA-ALG载药纳米粒的体外释药性能和对肝癌细胞的抑制作用.利用核磁、红外和元素分析技术对GA-ALG结构和GA取代度进行了表征;对GA-ALG载药纳米粒的形貌、粒径、表面Zeta电位等进行了测定,结果显示纳米粒具有较规则球形结构,其水合粒径为(214±11)nm.GA-ALG载药纳米粒在模拟生理条件下(pH7.4)可持续释药长达20天;MTT结果显示GA-ALG载药纳米粒对7703肝癌细胞的具有明显的杀伤作用.
In this study, glycyrrhetinic acid (GA), a liver-targeting molecule, was conjugated to natural polymeric sodium alginate (ALG) with biocompatibility and biodegradability. Glycyrrhetinic acid-modified alginic acid (GA-ALG). The broad-spectrum anti-cancer drug doxorubicin (DOX) was encapsulated to prepare liver-targeting drug-loaded nanoparticles. The in vitro drug release properties of GA-ALG drug- ALG structure and GA substitution degree were characterized by NMR, IR and elemental analysis techniques. The morphology, particle size and surface Zeta potential of GA-ALG drug-loaded nanoparticles were measured, The results showed that the nanoparticles had a regular spherical structure and the hydrated diameter was (214 ± 11) nm. The sustained release of the drug-loaded nanoparticles was up to 20 days under simulated physiological conditions (pH7.4) The results showed that GA-ALG drug-loaded nanoparticles have a significant killing effect on 7703 hepatoma cells.