Wu Jia-Hui, Wang Xiao-Juan, Li Shu-Juan, Ying Xiao-Ying, Hu Jing-Bo, Xu Xiao-Ling, Kang Xu-Qi, You Jian, Du Yong-Zhong
Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Road, Hangzhou, 310058, PR China.
Iran J Pharm Res. 2019 Spring;18(2):556-568. doi: 10.22037/ijpr.2019.1100651.
Sustained release of thermal-instable and water-soluble drugs with low molecule weight is a challenge. In this study, sodium bicarbonate was encapsulated in ethyl cellulose microspheres by a novel solid-in-oil-in-oil (S/O/O) emulsification method using acetonitrile/soybean oil as new solvent pairs. Properties of the microspheres such as size, recovery rate, morphology, drug content, and drug release behavior were evaluated to investigate the suitable preparation techniques. In the case of that the ratio of the internal and external oil phase was 1: 9, Tween 80 as a stabilizer resulted in the highest drug content (2.68%) and a good spherical shape of microspheres. After the ratio increased to 1: 4, the microspheres using Tween 80 as the stabilizer also had high drug content (1.96%) and exhibited a sustained release behavior, with 70% of drug released within 12 h and a sustained release of more than 40 h. Otherwise, different emulsification temperatures at which acetonitrile was evaporated could influence the drug release behaviour of microspheres obtained. This novel method is a potential and effective method to achieve the encapsulation and the sustained release of thermal-instable and water-soluble drugs with low molecule weight.
低分子量热不稳定且水溶性药物的持续释放是一项挑战。在本研究中，以乙腈/大豆油作为新的溶剂对，通过一种新型的油包固油包油（S/O/O）乳化方法将碳酸氢钠包封于乙基纤维素微球中。对微球的尺寸、回收率、形态、药物含量及药物释放行为等性质进行评估，以研究合适的制备技术。在内相和外相油相比例为1:9的情况下，吐温80作为稳定剂时药物含量最高（2.68%），且微球呈良好的球形。当比例增至1:4后，使用吐温80作为稳定剂的微球药物含量也较高（1.96%），并呈现出持续释放行为，12小时内70%的药物释放，且持续释放超过40小时。此外，乙腈蒸发时不同的乳化温度会影响所得微球的药物释放行为。这种新方法是实现低分子量热不稳定且水溶性药物包封及持续释放的一种潜在有效方法。
