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1、蚯蚓纤溶酶壳聚糖微球的制备及性质武金霞1,王英锐1,田志鹏1,李瑞1,张贺迎2(1.河北大学生命科学学院,河北保定071002;2.河北大学生物技术研究中心,河北保定071002)摘要:以蚯蚓纤溶酶为生物大分子模式药物,研究壳聚糖载药微球的制备方法及对药物活性和稳定性的影响。以壳聚糖为原料,采用超声乳化交联法制备壳聚糖微球,分别吸附和包埋蚯蚓纤溶酶。在油水体积比15/1,搅拌转速800r/min,1mL戊二醛作为交联剂,超声处理5min条件下乳化交联制备微球,包埋法具有较高的载药率和包封率,分别
2、达到52.6%和48.7%,具有一定的缓释效果,在72h药物累计释放率约为65%。用生理盐水溶出微球中的蚯蚓纤溶酶,电泳图谱显示,多数组分能被溶出,条带没有变化,在72h内,包埋法活性总溶出率达51.5%。关键词:蚯蚓纤溶酶;壳聚糖微球;载药率;包封率;溶出率中图分类号:Q55文献标志码:A文章编号:1000—1565(2011)04-0406-07PreparationofChitosanMicrosphereLoadedEarthwormFibrinolyticEnzymesandItsPr
3、opertiesWUJin-xia1,WANGYing-rui1,TIANZhi-peng1,LIRui1,ZHANGHe-ying2(1.CollegeofLifeScience,HebeiUniversity,Baoding071002,China;2.ResearchCenterforBiotechnology,HebeiUniversity,Baoding071002,China)Abstract:Tostudythepreparingmethodsofchitasonmicrosphe
4、resandinvestigatetheinfluenceindrugactivityandstabilitywhenearthwormfibrinolyticenzymes(EFEs)wasasbiomacromoleculemodeldrug.Thechitosanmicrosphereswerepreparedbyultrasonicemulsificationmethod,EFEswasencapsulatedandadsorbedintomicrospheresrespectively
5、.Theoptimizedfactorswereasfollows.V(O):V(W)was15/1,stirringspeedwas800r/min,adding1mLofGlutaraldehyde,ultrasonictreatmentfor5min.TheloadedrateandencapsulationefficiencyofthemicrosphereencapsulatedEFEsattheseconditionswere52.6%and48.7%respectively,the
6、microspherepocessedthesustainedreleasingproperty,thetotalreleasingratein72hourswereabout65%.PhysiologicalsalinewasusedtodissolvetheEFEsfrommicrosphere,thephotogramofPAGEindicatedthatmostoftheEFEscomponentscouldbedissolved,andnoobviouschangescouldbeob
7、served.ThedissolvedEFEsactivitywasdeterminedbyFolin-phenolmethod,theresultsshowedthatthetotaldissolutionrateofthemicrosphereencapsulatedEFEswas51.5%whendippedinphysiologicalsalinefor72hours.Keywords:earthwormfibrinolyticenzyme;chitosanmicrosphere;dru
8、gloadedrate;encapsulationefficiency;dissolutionrate收稿日期:2011—4—12基金项目:河北大学博士基金资助项目第一作者:武金霞(1966—),女,河北曲阳人,河北大学教授,博士,主要从事生物化学及基因工程药物研究.E-mail:wjx6@163.com9血栓病是严重危害人类健康的常见多发病,死亡率高、致残率高。当血栓发生后,最有效的治疗方法就是溶栓,近年来,以蚯蚓纤溶酶(earthwormfibrinolyticenzymes,EFEs)为主