丹参酮Ⅱ_A白蛋白纳米粒的制备及其体外抗肿瘤药效研究

Preparation and antitumor effects of tanshinone Ⅱ_A loaded albumin nanoparticles

采用高压均质法制备丹参酮Ⅱ_A白蛋白纳米粒,以粒径、包封率和载药量为评价指标,采用星点设计-效应面法优选处方,进而考察其体外抗肿瘤效果。结果表明,采用优选的处方制备的丹参酮Ⅱ_A白蛋白纳米粒形态为规则的圆球形,粒径分布均匀,平均粒径为(175.7±3.07)nm,包封率和载药量分别为90.8%±1.47%和5.52%±0.09%。对于人早幼粒细胞白血病NB4细胞,载丹参酮Ⅱ_A白蛋白纳米粒较游离药物有更优的抑瘤效果。白蛋白纳米粒制备工艺简便,可显著改善丹参酮Ⅱ_A的溶解度,有助于拓展其在抗血液肿瘤方面的应用。

In this study,the tanshinone ⅡAloaded albumin nanoparticles were prepared by high pressure homogenization method.The formulation was optimized by central composite design-response surface method（ CCD-RSM）,with the particle size,encapsulation efficiency,and drug loading as indexes to investigate their in vitro anti-tumor effect. The results showed that the prepared nanoparticles had uniformly spherical morphology and uniform particle size distribution. The average particle size,encapsulation efficiency and drug loading of nanoparticles were about（ 175. 7 ± 3. 07） nm,90. 8% ± 1. 47% and 5. 52% ± 0. 09%,respectively. Tanshinone ⅡA loaded albumin nanoparticles showed a more powerful antitumor effect than free tanshinone ⅡAfor human promyelocytic leukemia NB4 cells. The preparation method of the drug-loaded albumin nanoparticles was simple and easy,and can significantly improve the solubility of tanshinone ⅡA,so it was helpful to extend its application in therapies against hematological malignancies.