丹参酮ⅡA自纳米乳的制备及其质量的评价

Preparation and quality evaluation of tanshinone ⅡA self nano emulsifying drug delivery system

目的研制丹参酮ⅡA自纳米乳来增加药物的溶出率。方法采用伪三元相图法,以乳剂外观、粒径、Zeta电位为指标优选处方,采用HPLC测定丹参酮ⅡA,考察其药剂学特性。结果优选处方为Tween80-PEG400-MCT(31∶62∶7),载药量1.5 mg·m L-1,平均粒径42.63±1.80 nm,多分散系数PDI为0.16±0.037,Zeta电位为-12.35±0.96 m V。以0.5%Tween80为溶出介质,丹参酮ⅡA自纳米乳在1.5 h时的累积释药量即可达载药量的55%。结论丹参酮ⅡA自纳米乳可显著提高药物的溶出速率。

OBJECTIVE To develope tanshinone Ⅱ A （Tan Ⅱ A） self nano emulsifying drug delivery system to increase the drug dissolution rate. METHODS The formulation optimization was performed by Pseudo - ternary phase diagram and evaluated by the physical appearance,mean particle size and Zeta potential. An HPLC method was applied to determine Tan Ⅱ A to characterize the developed drug delivery system. RESULTS The optimized formulation composed of Tween80 - PEG400 - MCT （31 ： 62 ： 7 ）. In optimized formulation, the drug loading was 1.5 mg· mL^- 1 , and the mean particle size was 42.63 ± 1.80 nm, and the Zeta potential was - 12.35 ± 0.96 mV and the PDI was 0.16 ± 0. 037. The cumulative amount of drug release from the self nano emulsifying drug delivery system reached 55% of the drug loading in 1.5 hours when 0.5% Tween80 was served as dissolution medium. CONCLUSION The developed self - emulsifying nano emulsion formulation can increase the dissolution rate of Tan Ⅱ A.