RGD修饰树枝状高分子PAMAM药物靶向传输实验研究  

Modification of Polyamidoamine Dendrimer with RGD for Targeted Drug Delivery

作　　者：刘鉴峰[1] 刘金剑[1] 冯丽娜[1] 杨翠红[2] 褚丽萍[1] 孔德领[2] 

机构地区：[1]中国医学科学院放射医学研究所,天津市分子核医学重点实验室,天津300192 [2]南开大学生物活性材料教育部重点实验室,天津300071

出　　处：《南开大学学报（自然科学版）》2012年第6期17-22,共6页Acta Scientiarum Naturalium Universitatis Nankaiensis

基　　金：国家自然科学基金(81171371,20774050);天津市自然科学基金(09JCYBJC13400)

摘　　要：制备了RGD靶向修饰的聚酰胺-胺(PAMAM)树枝状聚合物,以阿霉素为药物模型研究了载体的载药性能、体外释放行为及对Hela细胞的毒性.利用激光共聚焦显微镜观察了Hela细胞对药物和材料的摄取行为.结果显示,载体具有良好的生物相容性,Hela细胞对PAMAM-Ac-FITC-RGD的摄取效率≥95%,而对PA-MAM-Ac-FITC的摄取效率<40%,293T细胞对两种材料的摄取效率均低于30%.阿霉素可以通过物理包埋的方法固定,其释放受pH、离子强度等因素的影响较大.共聚焦结果显示,载体可以在较短的时间内携带药物进入Hela细胞.RGD修饰PAMAM使载体获得了靶向性,提高了药物传输效率.The nano targeting carrier was synthesized by targeting agent RGD conjugated to modified ployamidoamine dendirmer（PAMAM-Ac-FITC-RGD）,the drug loading,release and cytotoxicity to Hela cells were studied with doxorubicin（DOX） as drug modle in vitro.Hela cells uptake of DOX and drug loaded carrier was also observed using confocal microscopy.The results indicated that PAMAM-Ac-FITC-RGD had good biocompatibility.The uptake efficiency of PAMAM-Ac-FITC-RGD（≥95%） by Hela cells was two fold higher than that of PAMAM-Ac-FITC（40%）,and more than threefold higher than the uptake of two conjugates by 293T cells（30%）.DOX can encapsulated to PAMAM-Ac-FITC-RGD,and ion concentration,pH and temperature could affect the release of DOX.The results of confocal microscopy showed that the carrier could facilitate drug to Hela cells in a short time.The modification of RGD to PAMAM make the carrer get targeting capability and improve its drug delivery efficiency.

关 键 词：纳米载体 RGD 树枝状高分子 靶向药物传输 

分 类 号：Q813[生物学—生物工程]