MUC1靶向性载紫杉醇超声造影剂的制备及体外靶向实验  

Preparation of MUC1-targeted and paclitaxel-loaded ultrasound contrast agent and experiment in vitro

作　　者：秦颢诚 武俊[2] 于明[1] 李洪娥[1] 刘燕[1] QIN Hao-cheng;WU Jun;YU Ming;LI Hong-e;LIU Yan(Department of Ultrasound,Lianyungang First People’s Hospital,Lianyungang Jiangsu 222061,China;Department of Ultrasound,the Second Affiliated Hospital of Dalian Medical University,Dalian Liaoning 116027,China)

机构地区：[1]连云港市第一人民医院超声科,江苏连云港222061 [2]大连医科大学附属第二医院超声科,辽宁大连116027

出　　处：《中国临床医学影像杂志》2021年第6期445-448,共4页Journal of China Clinic Medical Imaging

基　　金：国家自然科学基金(基金号:81501476);辽宁省自然科学基金(基金号:214023001)。

摘　　要：目的:制备MUC1靶向的载药超声造影剂(PTX-PLGA-Apt),并评价其在体外靶向能力及显影效果。方法:通过双乳化法及碳二亚胺法制备PTX-PLGA-Apt。检测该造影剂的一般性质,体外初步评价其靶向能力及细胞毒性,观察其体外超声显影情况。结果:PTX-PLGA-Apt的平均粒径为(328.79±43.57) nm,药物包封率及载药量分别为(85.1±4.28)%、(8.51±0.42)%,在体外可以被MCF-7细胞特异性结合,且对该细胞的杀伤作用显著。结论:成功制备出MUC1靶向的载紫杉醇超声造影剂,可与MCF-7细胞特异性结合并提高化疗药物对肿瘤细胞的杀伤效果。Objective: To prepare MUC1-targeted drug-loaded ultrasound contrast agent(PTX-PLGA-Apt) and evaluate its target seeking ability and imaging effect in vitro. Methods: Double emulsion method and carbon diimide method were used to prepare PTX-PLGA-Apt. The general properties of the contrast agent were tested, its targeting ability and cytotoxicity were preliminarily evaluated in vitro, and its ultrasound imaging was observed in vitro. Results: The average particle size of PTXPLGA-Apt was(328.79±43.57) nm, and the drug encapsulation rate and drug loading were(85.1±4.28)% and(8.51±0.42)%,respectively. It could be specifically bound by MCF-7 cells in vitro, and had significant killing effect on the cells. Conclusion: MUC1-targeted paclitaxel ultrasound contrast agent can bind specifically to MCF-7 cells and improve the killing effect of chemotherapy drugs on tumor cells.

关 键 词：造影剂 超声检查 

分 类 号：R981.9[医药卫生—药品] R445.1[医药卫生—药学]