3,5-二叔丁基水杨酸锌纳米粒的制备及其抗三阴性乳腺癌活性研究  

Preparation of 3,5-di-tert-butylsalicylate Zinc Nanoparticles and Its Inhibitory Effect on TNBC

作　　者：陈铭 王东 陈恒 范丽梅[1,2] 刘钰晨 柳昀熠 CHEN Ming;WANG Dong;CHEN Heng;FAN Limei;LIU Yuchen;LIU Yunyi(School of Medicine,Jianghan University,Wuhan 430056,Hubei,China;Cancer Institute,Jianghan University,Wuhan 430056,Hubei,China)

机构地区：[1]江汉大学医学部,湖北武汉430056 [2]江汉大学肿瘤研究所,湖北武汉430056

出　　处：《江汉大学学报(自然科学版)》2025年第1期56-62,共7页Journal of Jianghan University:Natural Science Edition

基　　金：国家自然科学基金项目(81602642);湖北省教育厅指导项目(B2019233);江汉大学基础性科研项目(2021jczx-002);江汉大学高层次人才培育项目(3015/06210046)。

摘　　要：目的3,5-二叔丁基水杨酸锌[Zn(DTBS)2]在水中的溶解度极低,易发生聚集沉淀而降低药效,为了克服这一缺陷,故制备可以提高原料药物生物利用度的3,5-二叔丁基水杨酸锌纳米粒(ZnNPs),并检测其对三阴性乳腺癌细胞的活性抑制作用。方法纳米沉淀法制得ZnNPs后,测定该纳米粒的形态、粒径、Zeta电位、包封率和载药量,MTS法检测它对人三阴性乳腺癌MDA-MB-231细胞的抑制作用。结果所得纳米粒呈大小均一的实心球状结构,粒径为(240±18)nm,ζ电位为(-35±8)mV,包封率为(82.66±1.98)%,载药量为(11.77±0.28)%。ZnNPs从50μmol/L的浓度开始,呈浓度和时间依赖性地抑制三阴性乳腺癌细胞活性,且相较于同样浓度的游离[Zn(DTBS)2],ZnNPs处理显示出更强的抗癌活性。结论Zn⁃NPs可增强Zn(DTBS)2对三阴性乳腺癌细胞活性的抑制作用。Objective Zinc 3,5-di-tert-butylsalicylate[Zn(DTBS)2]has extremely low solubility in water and is prone to aggregation and precipitation,which reduces its efficacy.To overcome this defect,zinc 3,5-di-tert-butylsalicylate nanoparticles(ZnNPs)were prepared to improve the bioavailability of the raw drug and investigate its inhibitory effect on the activity of triple-negative breast cancer cells.Methods After ZnNPs were prepared by nanoprecipitation,the morphology,particle size,zeta potential,encapsulation efficiency,and drug loading of the nanoparticles were determined,and its inhibitory effect on human triple-negative breast cancer cells MDA-MB-231 was detected by MTS assay.Results ZnNPs had a solid spherical structure of uniform size,with diameter of(240±18)nm,ζpotential of(-35±8)mV,encapsulation efficiency of(82.66±1.98)%,and drug loading of(11.77±0.28)%.ZnNPs inhibited the activity of triple-negative breast cancer cells in a concentration-and time-dependent manner from the concentration of 50μmol/L,and compared with the same concentration of free[Zn(DTBS)2],ZnNPs showed stronger anticancer activity.Conclusion ZnNPs can enhance the inhibitory effect of Zn(DTBS)2 on triple-negative breast cancer cell activity.

关 键 词：3 5-二叔丁基水杨酸锌 纳米粒 三阴性乳腺癌 纳米沉淀法 

分 类 号：R737.9[医药卫生—肿瘤] R979.1[医药卫生—临床医学]