盐酸普萘洛尔S-乙酰巯基丁二酸多孔淀粉酯微球的制备及其纤毛毒性和黏附性的研究  

Preparation of propranolol-carrying S-acetyl mercapto succinic porous starch microsphere and studies on its ciliary ciliotoxicity and mucoadhesive characteristics

作　　者：王霞[1] 李超[1] 冯川东[1] 陈鑫[1] 苏敏[1] 

机构地区：[1]第三军医大学药学院,重庆400038

出　　处：《华西药学杂志》2013年第1期38-41,共4页West China Journal of Pharmaceutical Sciences

基　　金：重庆市科技攻关项目(编号:CSTS 2010AC5027)

摘　　要：目的制备盐酸普萘洛尔S-乙酰巯基丁二酸多孔淀粉酯微球(Pro-SAMS),考察其用于鼻腔黏膜的纤毛毒性和黏膜黏附性。方法利用吸附法将Pro包合到被SAMS酯化后的多孔淀粉内,并且借助红外光谱仪、差示扫描量热仪(DSC),X-射线粉末衍射(XRPD)和扫描电镜(SEM)进行表征;通过测定在体蟾蜍上腭纤毛摆动持续时间评价载药微球的鼻纤毛毒性、纤毛的输送速率来评价载药微球的黏膜黏附性。结果当盐酸普萘洛尔与载体的比例为1∶2时,微球的载药率最高,可达13.91%;所制微球可显著降低盐酸普萘洛尔的鼻纤毛毒性,且具有良好的黏膜黏附性。结论 S-乙酰巯基丁二酸多孔淀粉酯微球是鼻腔给药系统的理想载体。OBJECTIVE To prepare the S-acetyl mercapto succinic porous starch microsphere carried propranolol（Pro-SAMS） and study its ciliotoxicity and mucoadhesion characteristics.METHODS Pro-SAMS porous starch microsphere was prepared by absorption and characterized by IR spectrum,differential scanning calorimetry（DSC）,X-ray diffraction（XRPD） and scanning electron microscopy（SEM）.Furthermore,the lasting time of ciliary movement was recorded with in situ toad palate model to evaluate the ciliotoxicity.To investigate its mucoadhesion properties,the mucociliary transport rate was recorded across a toad palate.RESULTS The maximum drug-loading was 13.91% when the PRO/carrier was 1：2.The characteristics of PRO-SAMSA porous starch microsphere were confirmed by IR spectrum,DSC,X-RPD and SEM.The PRO′s ciliotoxicity was reduced distinctly and mucoadhesion capacity was simutaneously increased after the formation of PRO-SAMSA porous starch microsphere.CONCLUSION SAMSA porous starch can be a novel ideal drug carrier for intranasal drug delivery systems.

关 键 词：盐酸普萘洛尔 微球 包合 纤毛毒性 黏附性 鼻腔给药系统 

分 类 号：R94[医药卫生—药剂学]