首页|雷帕霉素核壳型pH敏感递药系统制备及其对乳腺癌细胞的体外作用

雷帕霉素核壳型pH敏感递药系统制备及其对乳腺癌细胞的体外作用

Preparation of rapamycin-loaded core-shell pH-sensitive drug delivery system and its effect on breast cancer cells in vitro

扫码查看
目的 制备载雷帕霉素(RAPA)核壳型pH敏感递药系统,观察其对乳腺癌细胞的体外作用.方法 采用溶胶-凝胶法制备以脂质体包裹的介孔二氧化硅纳米粒(MSN),对MSN进行氨基化修饰后载入RAPA,通过薄膜分散法制备载RAPA的介孔二氧化硅核脂质纳米粒(RAPA-MSN-LN),对其包封率、形态、粒径、电位、稳定性和释放度进行评价.以乳腺癌MCF-7和4T1细胞为模型,采用噻唑蓝法观察RAPA-MSN-LN对乳腺癌细胞生长的抑制作用,通过流式细胞仪分析RAPA-MSN-LN对细胞凋亡的影响.结果 RAPA-MSN-LN制备成功,RAPA的包封率为(48.92± 1.50)%,平均粒径为(98.12±1.80)nm,多分散性指数为0.146±0.013,电位为(-18.4±1.2)mV.稳定性观察结果显示,RAPA-MSN-LN在4、25、37 ℃环境下和在血清中稳定性较好.体外释放实验证明,RAPA-MSN-LN具有显著的pH敏感性.体外抗肿瘤实验结果表明,RAPA-MSN-LN能有效抑制乳腺癌MCF-7、4T1细胞的生长并诱导细胞凋亡.结论 RAPA-MSN-LN具有较高的包封率及pH敏感性,体外抗肿瘤作用效果较好.
Objective To prepare a rapamycin(RAPA)-loaded core-shell pH-sensitive drug delivery system and investigate its effect on breast cancer cells in vitro.Methods Mesoporous silica nanoparticles(MSNs)encapsulated by liposomes were prepared using the sol-gel method,and RAPA was loaded after the MSNs were amino modified.Rapamycin-loaded mesoporous silica nanoparticles core-lipid shell nanoplatform(RAPA-MSN-LN)was prepared by thin-film dispersion method,and their encapsulation efficiency,morphology,particle size,potential,stability and release behavior were evaluated.Breast cancer cells MCF-7 and 4T1 were used as models,and the inhibitory effect of RAPA-MSN-LN on the growth of breast cancer cells was detected by the methyl thiazolyl tetrazolium method and the effect of RAPA-MSN-LN on cell apoptosis was analyzed by flow cytometry.Results RAPA-MSN-LN was successfully prepared.The encapsulation efficiency of RAPA was(48.92±1.50)%,the average particle size was(98.12±1.80)nm,the polydispersity index was 0.146±0.013,and the potential was(-18.4±1.2)mV.The stability observation showed that RAPA-MSN-LN was stable at 4,25,and 37℃ and in serum.The results of the release experiment in vitro showed that RAPA-MSN-LN had significant pH-sensitivity.The results of the anti-tumor experiment in vitro showed that RAPA-MSN-LN could effectively inhibit the growth of breast cancer cells MCF-7 and 4T1 and induce their apoptosis.Conclusion RAPA-MSN-LN has high encapsulation efficiency,pH-sensitivity and good anti-tumor effect in vitro.

rapamycinmesoporous silicapH-sensitive liposomesanti-cancer activity

王金梅、张凯、张颖、王爽、刘凡凡、何勐

展开 >

郑州大学附属郑州中心医院药学部,河南 郑州 450000

雷帕霉素 介孔二氧化硅 pH敏感脂质体 抗肿瘤活性

2024

新乡医学院学报
新乡医学院

新乡医学院学报

CSTPCD
影响因子:0.999
ISSN:1004-7239
年,卷(期):2024.41(4)
  • 19