含RGD修饰的丹参酮ⅡA多级靶向纳米粒的制备及工艺优化

Preparation and optimization of TSⅡA-loaded mPEG-PLGAPLL-cRGD nanoparticles

目的探讨丹参酮ⅡA多级靶向纳米粒的制备及其工艺优化。方法采用乳化溶剂蒸发法制备丹参酮ⅡA多级靶向纳米粒;考察单因素在纳米粒制备过程中的影响,包括TSⅡA载药纳米粒中的药物浓度、乳化剂浓度、有机相/外水相、超声时间和强度等的改变;并通过正交设计优化TSⅡA多级靶向纳米粒的制备工艺。结果本实验成功制备了含RGD修饰的丹参酮ⅡA多级靶向纳米粒,优选工艺参数为:药物浓度1mg/mL,载体材料浓度20mg/mL,有机相/外水相为1∶10,超声强度和时间分别为200W,20×5s。结论此丹参酮ⅡA多级靶向纳米粒的制备工艺切实可行。所制备的TNP包封率和载药量较高,为丹参酮ⅡA的临床应用提供了更广阔的前景。

Objective To study the targeting efficacy of Tanshinone Ⅱ A（TSⅡA） nanoparticles（TNP）. Methods TNP was prepared by a oil-in-water （O/W） emulsion/solvent evaporation method and orthogonal design for optimization of formulation and technology. Results The optimum formula and preparation method NP were： TSIIA 1mg/Ml, mPEG-PLGA-PLL 20mg/mL, O/W 1 ︰ 10, with sonicate time of 20×5s and sonicate intensity of 200W. Conclusion The TNP has high entrapment efficiency and drug loading, which provides an extensive prospect for clinical application of TSⅡA.