藤黄酸聚乳酸纳米粒的研制

Study on Gambogic Acid-loaded Polylacticacid Nanoparticles

以新型材料聚乳酸(PLA)为载体,研制出质量稳定的藤黄酸聚乳酸纳米粒(GA-PLA-NPs)乳液制剂,并对其安全性进行评价。采用改良的溶剂蒸发法制备藤黄酸聚乳酸纳米粒(GA-PLA-NPs);用透射电子显微镜(TEM)观察纳米粒的形态;用激光粒度分析仪测定其平均粒径大小和分布;经超速离心后用紫外分光光度计测定纳米粒的包封率与载药量;考察藤黄酸纳米粒的体外释放特性;经急性毒性实验考察藤黄酸纳米粒的安全性。得到确定处方工艺为:水相∶有机相为2∶1(v/v),表面活性剂在有机相中的浓度为0.5%(w/v),藤黄酸(GA)在有机相中的浓度为0.1%(w/v),GA∶PLA为1∶4(w/w)。处方条件下制备的纳米粒平均粒径为51.36nm;平均包封率与载药量分别为98.87%和13.3%;藤黄酸纳米粒的体外释药分为两相:突释期和缓释期;急性毒性试验测得藤黄酸纳米粒的ID50为26.3mg/kg。制备的藤黄酸聚乳酸纳米粒(GA-PLA-NPs)质量稳定、分散性良好;聚乳酸可能成为藤黄酸的新型载体。

Gambogic acid-loaded polylacticacid nanoparticles （GA-PLA-NPs） were prepared by modified emulsification solvent diffusion. The shape of nanoparticles was observed by transmission electron microscope （TEM）. The size distribution and mean diameter were measured by laser particle size analyzer. The entrapment efficiency and content of drug loading were determined by Ultraviolet Spectrophotometer after uhracentrifugation.GA-PLA-NPs release behavior in vitro was carried out. The acute toxicity were carried out to study the security of GA-PLA-NPs. The preparation process adapted to the formulation was as follows： the volume ratio of the aqueous and organic was 2：1 （ v/v）, the suffactant concentration in aqueous was 0. 5% ,the drug concentration in organic was 0.1% （ w/v）, GA： PLA was 1 ： 4（w/w）. The mean diameter was 51.36nm for the nanoparticles prepared by above conditions. The entrapment efficiency and content of drug loading were 98.87 % and 13.3 %. The release behavior of drug in vitro showed an initial burst effect with subsequently a slower rate stage. The LDSO value of GA-PLA-NPs on mouse was 26.3 mg/kg. The results showed that the GA-PLA-NPs were well prepared with stable quality and high dispersion. PLA-NPs might be used as a new carrier for gambogic acid.