Chongqing Academy of Chinese Materia Medica, Chongqing, 400065, People's Republic of China.
Shaanxi University of Chinese Medicine, Xianyang, 712046, People's Republic of China.
Drug Des Devel Ther. 2021 Apr 21;15:1623-1631. doi: 10.2147/DDDT.S294314. eCollection 2021.
This study aims to investigate the preparation of sustained-release microcapsules of salvianolic acid.
The stability of salvianolic acid microcapsules was improved, and the time of action was prolonged in the present study. This was prepared using the spray-drying method, with chitosan as the carrier. In the preparation process, the prescription and process were optimized by L9 (34) using an orthogonal design, with yield and drug loading as indexes, in order to obtain optimum conditions.
The optimal process and prescription for the preparation of salvianolic acid microcapsules were found to be as follows: mass concentration of chitosan, 1.5%; mass ratio of salvianolic acid to chitosan, 1:3; inlet air temperature, 190°C; and peristaltic pump speed, 300 mL·h-1. The surface of the microcapsules was round, the drug loading was 25.99% ± 2.14%, the yield was 51.88% ± 2.84%, the entrapment efficiency was 86.21% ± 2.89%, and the average particle size was 105.6 ± 2.56 nm. The microcapsules in vitro had certain sustained release characteristics. The internally fitted first-order release model equation was ln(1-Q) = -0.236 t + 4.591 7, r = 0.920. In addition, the results of differential scanning calorimetry show that the properties of salvianolic acid were not changed by the microcapsules.
Sustained-release microcapsules of salvianolic acid can be successfully prepared by adopting marine polysaccharide as a carrier.
本研究旨在探讨丹酚酸长效缓释微囊的制备方法。
采用喷雾干燥法，以壳聚糖为载体，提高丹酚酸微囊的稳定性，延长其作用时间。在制备过程中，采用 L9（34）正交设计，以收率和载药量为指标，对处方和工艺进行优化，以获得最佳条件。
确定了丹酚酸微囊的最佳制备工艺和处方条件为：壳聚糖质量浓度 1.5%；丹酚酸与壳聚糖质量比 1：3；进风温度 190℃；蠕动泵转速 300 mL·h-1。微囊表面圆整，载药量为 25.99%±2.14%，收率为 51.88%±2.84%，包封率为 86.21%±2.89%，平均粒径为 105.6±2.56nm。微囊体外具有一定的缓释特性，拟合的内装式一级释放模型方程为 ln(1-Q)=-0.236t+4.5917，r=0.920。此外，差示扫描量热法结果表明，微囊未改变丹酚酸的性质。
采用海洋多糖作为载体可成功制备丹酚酸长效缓释微囊。
