丹参酮ⅡA和芍药苷复合脂质体的制备及其质量评价

Preparation and Quality Evaluation of Tanshinone ⅡA and Paeoniflorin Complex Liposome

目的:制备丹参酮ⅡA和芍药苷复合脂质体来提高丹参酮ⅡA的溶解度和稳定性,改善它的释放行为。方法:本实验采用乙醇注入法制备丹参酮ⅡA和芍药苷复合脂质体,通过单因素考察、正交实验设计筛选最优处方。采用超滤离心法测定丹参酮ⅡA的包封率,采用激光粒度仪和扫描电子显微镜测定脂质体的粒径和形态,用小杯法研究其体外释放行为。结果:最优处方中丹参酮ⅡA的包封率为86.7%,制备所得的丹参酮ⅡA和芍药苷复合脂质体为微橙色透明溶液,平均粒径为29.49nm,PDI值为0.159,Zeta电位为-30.3mV,制得脂质体在扫描电镜下呈圆球形,长期稳定性实验结果表明其三个月内的稳定性较好,体外释放实验结果表明在12小时释放了90.0±3.22%。结论:本实验通过脂质体为载体,将中药复方中常见的两种药物单体结合在一种制剂中,且制备方法简便,粒径均匀,稳定性较好,相较于丹参酮ⅡA原料药有一定的缓释效果。

Objective:To improve the solubility, stability and release behavior of Tanshinone ⅡA, the liposome(TSN-PAE LP), Tanshinone ⅡA and paeoniflorin complex were prepared. Methods: TSN-PAE LP was prepared by ethanol injection method. The optimal prescription was screened by using single factor investigation and orthogonal experimental design. The encapsulation efficiency of TSN-PAE LP was determined by ultrafiltration centrifugation. The particle size and morphology of TSN-PAE LP was determined by laser particle size analyzer and scanning electron microscopy. The in-vitro release behavior was studied by the small cup method. Results: The encapsulation efficiency of Tanshinone ⅡA in the optimal prescription was 86.7%. The TSN-PAE LP was slightly orange transparent solution which the average particle size, PDI value and zeta potential was 29.49 nm, 0.159, and-30.3 mV, respectively. The TSN-PAE LP was spherical under SEM. The long-term stability results showed that the stability was good within three months. The in-vitro release showed that a total release of Tanshinone ⅡA was 90.0 ± 3.22% within 12 hours. Conclusion: Two drug, commonly used in traditional Chinese medicine, were combined into one preparation through liposome as carrier. Comparsion with Tanshinone ⅡA crude drug,the TSN-PAE LP showed sustained-release effect and the preparation method, particle size and stability is simple, uniform and good, respectively.