Dialdehyde starch nanoparticles as antitumor drug delivery system:An in vitro,in vivo,and immunohistological evaluation  

作　　者：XIAO SuYao LIU XuanMing TONG ChunYi ZHAO LiChao LIU XiaoJuan ZHOU AiMei CAO Yong 

机构地区：[1]College of Food Science,South China Agricultural University.Guangzhou 510642,China [2]Institute of Life Science and Biotechnology,Hunan University,Changsha 410082,China

出　　处：《Chinese Science Bulletin》2012年第24期3226-3232,共7页

基　　金：supported by the National Natural Science Foundation of China (31100433)

摘　　要：Sustaining the release of therapeutic nanoparticles in a cell-, tissue-, or disease-specific manner is a potentially powerful technology. A new drug carrier-dialdehyde starch nanoparticle (DASNP) that can sustain the loading and release of 5-fluorouracil (5-Fu) antitumor drug is reported in this study. IR spectrophotometer and 1H NMR confirmed the formation of aldehyde groups, and scan electron microscope determinations showed that the dialdehyde starch nanoparticles obtained had an average diameter of 90 nm. 5-Fu, the model drug, was conjugated into nanoparticles by aldehyde groups. These 5-Fu-binding nanoparticles significantly enhanced breast cancer cell (MCF-7) inhibition in vitro compared with free 5-Fu. After subcutaneous 0 injection in the breast tumor-loaded rats, 5-Fu-DASNP exhibited remarkable tumor-inhibitory efficacy determined by measuring tumor weight in vivo. The tumor inhibition of 5-Fu-DASNP was 61%±6%, whereas that of free 5-Fu was only 42%±4%. Bcl-2/Bax immunohistochem-istry studies indicated that 5-Fu-DASNP remarkably induced tumor tissue necrosis. These results demonstrated that the DASNP prepared in this work is a potentially effective drug carrier.Sustaining the release of therapeutic nanoparticles in a cell-, tissue-, or disease-specific manner is a potentially powerful techno- logy. A new drug carrier-dialdehyde starch nanoparticle （DASNP） that can sustain the loading and release of 5-fluorouracil （5-Fu） antitumor drug is reported in this study. IR spectrophotometer and IH NMR confirmed the formation of aldehyde groups, and scan electron microscope determinations showed that the dialdehyde starch nanoparticles obtained had an average diameter of 90 nm. 5-Fu, the model drug, was conjugated into nanoparticles by aldehyde groups. These 5-Fu-binding nanoparticles significantly en- hanced breast cancer cell （MCF-7） inhibition in vitro compared with free 5-Fu. After subcutaneous 0 injection in the breast tu- mor-loaded rats, 5-Fu-DASNP exhibited remarkable tumor-inhibitory efficacy determined by measuring tumor weight in vivo. The tumor inhibition of 5-Fu-DASNP was 61%-＋6%, whereas that of free 5-Fu was only 42%＋4%. Bcl-2/Bax immunohistochem- istry studies indicated that 5-Fu-DASNP remarkably induced tumor tissue necrosis. These results demonstrated that the DASNP prepared in this work is a potentially effective drug carrier.

关 键 词：抗癌药物 纳米颗粒 双醛淀粉 体外抑制 输送系统 免疫组化 体内 BCL-2/BAX 

分 类 号：TQ460.1[化学工程—制药化工]