壳聚糖-海藻酸钠靛玉红自微乳缓释微囊制备、评价及体外释放的研究

Preparation,Evaluation and in vitro Release on Chitosan Alginate Sustained Release Microcapsule of Indirubin Self Microemulsion

以靛玉红自微乳为囊心物,壳聚糖和海藻酸钠为囊材,采用复凝聚法制备壳聚糖-海藻酸钠靛玉红自乳化缓释微囊,通过正交实验和单因素考察确定壳聚糖-海藻酸钠靛玉红缓释微囊的最佳制备工艺。并以载药量、包封率为评价指标对其进行质量评价,同时以体外释放度评价其释药性能。壳聚糖-海藻酸钠靛玉红缓释微囊的最佳工艺是海藻酸钠的浓度为1.5%,靛玉红自微乳体积、海藻酸钠体积、壳聚糖质量三者比例为1∶1∶0.5,氯化钙浓度的最佳浓度为2.0%。采用该工艺制备的微囊载药量为0.0416%、包封率为79.2%,体外释放24 h累积释放率为(97.1±2.68)%。该微囊的释放符合Higuchi方程和一级释药模型,具有较好的缓释作用。

In this study,indirubin self-microemulsion was used as core material, chitosan and sodium alginate were used as wall materials to prepare ehitosan-alginate indirubin self-emulsifying microcapsules by complex coacervation method. The preparation process was optimized by single factor and orthogonal experiments. Then the quality evaluation was carried out with the drug loading and encapsulation efficiency. At the same time, the drug release property was evaluated with the drug release in vitro. The optimal preparation process was determined as follows ： The concentration of sodium alginate was 1.5% , the proportion of indirubin self-microemulsion volume, sodium alginate volume and chitosan mass was 1： 1：0.5 ,the optimal concentration of calcium chloride was 2%. The drug loading rate and encapsulation rate of microcapsules prepared by the optimized process was 0.0416% and 79.2% , respectively. The cumulative release rate of 24 h in vitro was （97.1 ± 2.68 ） %. The release of the microcapsules conformed to the Higuchi equation and one-order kinetics, hence it had a better sustained release effect.