紫杉醇甘草次酸修饰透明质酸纳米粒的制备及性能研究
Preparation and properties of paclitaxel-loaded glycyrrhetinic acid-modified hyaluronic acid nanoparticles
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摘要: 优化紫杉醇甘草次酸修饰透明质酸（PTX/GA-HA）纳米粒的载药工艺，并系统评价其体内外特性。以载药量、包封率为评价指标，通过单因素考察优化甘草次酸修饰透明质酸纳米粒的载药工艺。制得的纳米粒粒径为（321.2±8.2）nm，荷负电；载药量和包封率分别为（31.2±0.8）%和（90.3±1.6）%。体外释放动力学研究显示，在偏酸性介质中，PTX/GA-HA纳米粒下具有更快的释药速度。同时，MTT实验显示其对多种肿瘤细胞具有杀伤作用，尤其对HepG2细胞的生长抑制作用最强。此外，细胞摄取实验表明，GA-HA纳米粒易被肿瘤细胞摄取。因此，PTX/GA-HA纳米粒具有优良的体内外特性，其成功制备将有助于提高抗肿瘤药物的肿瘤靶向治疗效果。Abstract: Taking the drug-loading and entrapment efficiency as assessment indexes,we determined the process to load paclitaxel (PTX) using glycyrrhetinic acid-modified hyaluronic acid (GA-HA) nanoparticles by the single factor method.GA-HA nanoparticles could encapsulate PTX up to (31.2±0.8)%,with entrapment efficiency of (90.3±1.6)% .The particle size of PTX-loaded nanoparticles negatively charged was (321.2±8.2) nm.In vitro release of drugs from nanoparticles was investigated.Sustainable release of PTX/GA-HA nanoparticles was faster in acidic environment.From the cytotoxicity test,it was found that PTX/GA-HA nanoparticles exhibited strong cytotoxicity to many cells,especially in hepatoma cells.The cellular uptake of GA-HA nanoparticles was also investigated.When cancer cells over-expressing CD44 (the receptor for HA) were treated with fluorescently labeled GA-HA nanoparticles,stronger fluorescence signals were observed compared to free FITC.These results suggest that GA-HA nanoparticles have the potential as a novel polymer carrier of drugs for cancer therapy.
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Keywords:
- polymer nanoparticles /
- glycyrrhetinic acid /
- hyaluronic acid /
- paclitaxel /
- tumor targeting
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