国际医药卫生导报
國際醫藥衛生導報
국제의약위생도보
INTERNATIONAL MEDICINE & HEALTH GUIDANCE NEWS
2012年
14期
1999-2003
,共5页
壳聚糖%地塞米松%前药%pH敏感%纳米粒子
殼聚糖%地塞米鬆%前藥%pH敏感%納米粒子
각취당%지새미송%전약%pH민감%납미입자
Chitosan%Dexamethasone%Prodrug%pH sensitve%Nanopartical
[目的]合成具有pH敏感、缓释特性的壳聚糖-地塞米松前药,通过透析法制备前药胶束纳米粒子.[方法]通过缩合反应将壳聚糖与地塞米松通过腙键共价连接,制备壳聚糖负载的地塞米松前药,并通过核磁氢谱对其进行结构表征;通过透析法制备壳聚糖-地塞米松胶束纳米粒子,并用动态光散射仪和透射电镜考察粒子的粒径和形貌;考察壳聚糖-地塞米松pH敏感型纳米胶束前药在不同pH缓冲液中的释药特性.[结果]合成的前药鉴定为预期产物.通过透析法制得的前药纳米粒子粒径在100~250 nm之间;该前药在pH=5.8条件下的释放速率要快于pH=7.4条件下的释放速率,具有pH敏感性.[结论]成功合成了壳聚糖-地塞米松前药,通过透析法成功制备了前药胶束纳米粒子,该前药具有在低pH条件下释放较快的pH敏感性.
[目的]閤成具有pH敏感、緩釋特性的殼聚糖-地塞米鬆前藥,通過透析法製備前藥膠束納米粒子.[方法]通過縮閤反應將殼聚糖與地塞米鬆通過腙鍵共價連接,製備殼聚糖負載的地塞米鬆前藥,併通過覈磁氫譜對其進行結構錶徵;通過透析法製備殼聚糖-地塞米鬆膠束納米粒子,併用動態光散射儀和透射電鏡攷察粒子的粒徑和形貌;攷察殼聚糖-地塞米鬆pH敏感型納米膠束前藥在不同pH緩遲液中的釋藥特性.[結果]閤成的前藥鑒定為預期產物.通過透析法製得的前藥納米粒子粒徑在100~250 nm之間;該前藥在pH=5.8條件下的釋放速率要快于pH=7.4條件下的釋放速率,具有pH敏感性.[結論]成功閤成瞭殼聚糖-地塞米鬆前藥,通過透析法成功製備瞭前藥膠束納米粒子,該前藥具有在低pH條件下釋放較快的pH敏感性.
[목적]합성구유pH민감、완석특성적각취당-지새미송전약,통과투석법제비전약효속납미입자.[방법]통과축합반응장각취당여지새미송통과종건공개련접,제비각취당부재적지새미송전약,병통과핵자경보대기진행결구표정;통과투석법제비각취당-지새미송효속납미입자,병용동태광산사의화투사전경고찰입자적립경화형모;고찰각취당-지새미송pH민감형납미효속전약재불동pH완충액중적석약특성.[결과]합성적전약감정위예기산물.통과투석법제득적전약납미입자립경재100~250 nm지간;해전약재pH=5.8조건하적석방속솔요쾌우pH=7.4조건하적석방속솔,구유pH민감성.[결론]성공합성료각취당-지새미송전약,통과투석법성공제비료전약효속납미입자,해전약구유재저pH조건하석방교쾌적pH민감성.
[Objective]To synthesise the prodrug of chitosan-dexamethasone with pH sensitive release property.[Methods]The chitosan-dexamethasone prodrug was prepared by covalently linking via hydrazone bonds,and the structure of the prodrug was verified by 1H-NMR.The nanoprodrug was prepared by dialyse method,and the size and morphology were observed by dynamic light scattering and transmission electron microscope.The drug release in different pH of the prodrug was evaluated.[Results]The prodrug was synthesized and confirmed as expected.The size of the prodrug nanoparticle was about 100 ~ 250 nm,and the prodrug realeased faster in pH 5.8 than in pH 7.4 PBS solution.Conclsion The pH sensitve chitosan-dexamethasone prodrug is synthesized successfully,which has potential application in the rheumatoid arthritis treatment.