摘要
目的观察载多烯紫杉醇及酞菁锌并靶向乳腺癌多功能分子探针的体外光声显像特性及寻靶能力。方法采用双乳化法及碳二亚胺法制备载多烯紫杉醇及酞菁锌并连接RDG靶向肽的多功能分子探针。检测探针的一般物理特性、多烯紫杉醇及酞菁锌包封率及载药量、与RGD连接情况及体外寻靶能力,观察其体外光声显像情况、体外释放特性及体外抑制乳腺癌细胞的能力。结果成功制备靶向载多烯紫杉醇及酞菁锌的多功能分子探针,平均粒径(266.00±65.85)nm,表面电位(-29.20±6.27)mV;多烯紫杉醇包封率及载药量分别为(88.00±0.32)%、(34.92±0.02)μg/mg,酞菁锌包封率及载药量分别为(97.25±0.22)%、(30.87±0.11)μg/mg;靶向载多烯紫杉醇及酞菁锌纳米粒具有一定缓释效应,且呈明显光声信号,并随酞菁锌含量增加而增强。流式细胞仪检测RGD肽与靶向载多烯紫杉醇及酞菁锌纳米粒连接率为89.19%。激光辐照靶向载多烯紫杉醇及酞菁锌纳米粒后,乳腺癌细胞凋亡率明显增高。结论载多烯紫杉醇及酞菁锌并靶向乳腺癌多功能分子探针呈明显光声信号,并具备乳腺癌细胞靶向能力,可通过光声介导抑制乳腺癌细胞增殖。
Objective To investigate the targeting ability and photoacoustic imaging of novel nanoparticle probe loaded with ZnPc and docetaxel.Methods The polymeric nanoparticles probe loaded with ZnPc and docetaxel were fabricated using double emulsion method.RGDfK was modified on the surface for breast carcinoma targeting by carbodiimide method.The encapsulating ratio（ER）and drug loading（DL）of ZnPc and docetaxel were assessed.The modification rate and targeting ability of molecular probe were tested in vitro,and the photoacoustic imaging and drug release profiles were observed.Results The probes were loaded with ZnPc and docetaxel efficiently and successfully.The size of novel nanoparticle loaded with ZnPc and docetaxel was（266.00±65.85）nm,and the surface potential was（-29.20±6.27）mV.ER and DL of docetaxel was（88.00±0.32）% and（34.92±0.02）μg/mg,of ZnPc was（97.25±0.22）% and（30.87±0.11）μg/mg,respectively. The probes had certain sustained slow-release effect and showed obvious photoacoustic signals,which enhanced with the increase of the content of ZnPc.Flow cytometry detection results showed that the RGDfk modification rate was 89.19%.The apoptotic rate of novel nanoparticle loaded with ZnPc and docetaxel targeting breast carcinoma increased after the laser irradiation in vitro.Conclusion The new polymeric multifunctional nanoparticles probe has an ideal size and good photoacoustic signals,also the ability to target breast carcinoma cells and inhibit the proliferation of breast carcinoma cells efficiently.
作者
喻滔
黄晓玲
曹阳
陈瑜莉
冉海涛
YU Tao;HUANG Xiaoling;CAO Yang;CHEN Yuli;RAN Haitao(Department of Uhrasound,the First Affiliated Hospital of Chongqing Medical University,Chongqing 400016,China;Institute of Uhrasound Imaging,Chongqing Medical University,Chongqing Key Laboratory of Uhrasound Molecular Imaging,Chongqing 400016,China)
出处
《中国介入影像与治疗学》
CSCD
北大核心
2018年第5期295-300,共6页
Chinese Journal of Interventional Imaging and Therapy
基金
国家自然科学基金青年基金(81401503)
中国博士后科学基金(2015T80963
2016M590869)
重庆市博士后科学基金(Xm2015089)
重庆市高校创新团队建设计划(CXTDG201602007
KJTD201303)
关键词
乳腺肿瘤
光声成像
酞菁锌
靶向纳米探针
Breast neoplasms
Photoacoustic imaging
Zinc phthalocyanine
Targeted nanoparticle probe
