中国药科大学学报2024，Vol.55Issue(3)：381-389,9.DOI:10.11665/j.issn.1000-5048.2023102501
高载药量斑蝥素聚合物胶束递送系统制备及其抗乳腺癌研究
Preparation of high-drug-loading cantharidin polymer micelle delivery system and its anti-breast cancer activity
摘要
Abstract
The aim of this study was to prepare a high drug-carrying capacity micellar drug delivery system(CTD@Sol)of the polymer zebra tetracycline and to preliminarily investigate the feasibility of this drug delivery system for the treatment of breast cancer.Firstly,CTD@Sol was prepared using sol as the carrier material and CTD as the model drug,and its pharmacological properties such as appearance and morphology,particle size,potential and in vitro release were evaluated.The growth inhibitory and apoptotic effects of CTD@Sol on breast cancer(4T1)cells were investigated by MTT assay and Annexin V-FITC/PI double staining assay;the uptake efficiency of 4T1 to this delivery system was investigated by flow cytometry;and the in vivo tissue distribution of the delivery system and the targeting of tumour tissues were investigated by small animal in vivo imaging technique.The results showed that CTD@Sol appeared as a light pale blue creamy white colour,with an average particle size of(159.73±1.96)nm,a PDI of 0.198±0.006,Zeta potential of-(47.60±1.77)mV,an encapsulation rate of(90.29±1.69)%and a drug loading capacity of(45.00±0.84)%;the in vitro release and haemolysis experiments showed that the drug release rate of CTD@Sol in acidic environment(pH 5.5)was significantly faster than that in neutral environment(pH 7.4),suggesting that the system is acid-sensitive and has good biosafety under endocytosed pH conditions.Cellular uptake,cytotoxicity and apoptosis experiments showed that CTD@Sol was more lethal to 4T1 cells,and the sol-gel polymer micelles as a drug delivery vehicle could significantly improve the cellular uptake efficiency of the drug;in vivo experiments showed that the delivery system had a significant targeting effect on tumour tissues.In conclusion,this study has successfully produced a CTD@Sol drug delivery system with high drug loading capacity(>45%),good pharmacological performance,strong targeting and biosafety,which has the potential to be used in the treatment of breast cancer.关键词
斑蝥素/聚合物胶束给药系统/抗乳腺癌/靶向性Key words
cantharidin/polymeric micelle delivery system/anti-breast cancer/targeted分类
医药卫生引用本文复制引用
刘丝露,白云,王建华,张可青,孙艳雪,张可欣,徐鹏程..高载药量斑蝥素聚合物胶束递送系统制备及其抗乳腺癌研究[J].中国药科大学学报,2024,55(3):381-389,9.基金项目
内蒙古自治区高校青年科技英才项目(No.NJYT22007) （No.NJYT22007）
内蒙古自治区科技攻关项目(No.2019GG035) （No.2019GG035）
内蒙古医科大学科技转化项目(No.YKD2020CGZH003) This study was supported by the Program for Young Talents of Science and Technology in Universities of Inner Mongolia Autonomous Region(No.NJYT22007) （No.YKD2020CGZH003）
the Science and Technology Research Projects of Inner Mongolia Autonomous Region(No.2019GG035) （No.2019GG035）
and the Science and Technology Transformation Project of Inner Mongolia Medical University(No.YKD2020CGZH003) （No.YKD2020CGZH003）
