[1]王金梅,张凯,张颖,等.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[J].新乡医学院学报,2024,(4):316-321.[doi:10.7683/xxyxyxb.2024.04.003]
　WANG Jinmei,ZHANG Kai,ZHANG Ying,et al.Preparation of rapamycin-loaded core-shell pH-sensitive drug delivery system and its effect on breast cancer cells in vitro[J].Journal of Xinxiang Medical University,2024,(4):316-321.[doi:10.7683/xxyxyxb.2024.04.003]
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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
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《新乡医学院学报》[ISSN:1004-7239/CN:41-1186/R]

卷:
期数:
2024年4
页码:
316-321
栏目:
基础研究
出版日期:
2024-04-05

文章信息/Info

Title:
Preparation of rapamycin-loaded core-shell pH-sensitive drug delivery system and its effect on breast cancer cells in vitro
作者:
王金梅; 张凯; 张颖; 王爽; 刘凡凡; 何勐
（郑州大学附属郑州中心医院药学部，河南　郑州　450000）
Author(s):
WANG Jinmei; ZHANG Kai; ZHANG Ying; WANG Shuang; LIU Fanfan; HE Meng
(Department of Pharmacy,Zhengzhou Central Hospital Affiliated to Zhengzhou University,Zhengzhou 450000,Henan Province,China)
关键词:
雷帕霉素; 介孔二氧化硅; pH敏感脂质体; 抗肿瘤活性
Keywords:
rapamycin; mesoporous silica; pH-sensitive liposomes; anti-cancer activity
分类号:
R737.9
DOI:
10.7683/xxyxyxb.2024.04.003
文献标志码:
A
摘要:
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。
Abstract:
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.

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更新日期/Last Update: 2024-04-05