李菲菲, 张馨欣, 郭仕艳, 甘 勇, 李 娟. pH敏感性的脂质-介孔硅核/壳纳米粒作为抗肿瘤药物新型载体的初步研究J. 药学学报, 2013,48(2): 291-297.
引用本文: 李菲菲, 张馨欣, 郭仕艳, 甘 勇, 李 娟. pH敏感性的脂质-介孔硅核/壳纳米粒作为抗肿瘤药物新型载体的初步研究J. 药学学报, 2013,48(2): 291-297.
shu
LI Fei-fei, ZHANG Xin-xin, GUO Shi-yan, GAN Yong, LI Juan. Preliminary study on pH-sensitive lipid bilayer-coated mesoporous silica nanoparticles as a novel drug carrier for antitumor drugJ. 药学学报, 2013,48(2): 291-297.
Citation: LI Fei-fei, ZHANG Xin-xin, GUO Shi-yan, GAN Yong, LI Juan. Preliminary study on pH-sensitive lipid bilayer-coated mesoporous silica nanoparticles as a novel drug carrier for antitumor drugJ. 药学学报, 2013,48(2): 291-297.
shu

pH敏感性的脂质-介孔硅核/壳纳米粒作为抗肿瘤药物新型载体的初步研究

Preliminary study on pH-sensitive lipid bilayer-coated mesoporous silica nanoparticles as a novel drug carrier for antitumor drug

    摘要
  • 摘要:

    本文拟构建一种具有pH敏感性的脂质−介孔硅核/壳纳米粒 (lipid bilayer-coated mesoporous silica nanoparticles, LMSNs) 以提高抗肿瘤药物对肿瘤细胞的杀伤活性。采用水热−薄膜水化分散法合成制备了包载盐酸伊立替康 (irinotecan, CPT-11) 的脂质−介孔硅核/壳纳米粒 (lipid coated mesoporous silica nanoparticles loaded with CPT-11, CPT-11-LMSNs), 并对其进行了形态、粒度和释放度的表征。同时, 以人乳腺癌细胞MCF-7为细胞模型, 考察了载体的细胞摄取定位、药物胞内蓄积量和抗肿瘤活性。研究结果表明: LMSNs在透射电镜下呈圆整球形, 平均粒径为 (120.27 ± 5.91) nm。载体在体外模拟正常生理环境中CPT-11泄露量低, 而在模拟肿瘤胞内环境中快速释药, 表明该载体的释药行为具有pH响应性。另外, LMSNs可有效提高MCF-7细胞对药物的摄取量, 显著增加CPT-11对肿瘤细胞的杀伤力, 将CPT-11介孔硅纳米粒 (CPT-11-MSNs) 的胞内药物累积量提高2.1倍, 半数抑制浓度 (IC50) 降低1.4倍。

     

    Abstract:

    This study plans to prepare lipid bilayer-coated mesoporous silica nanoparticles (LMSNs) which are pH sensitive with core-shell structure to improve the tumor cell lethality of antitumor drug.  The lipid coated mesoporous silica nanoparticles loaded with irinotecan (CPT-11) (CPT-11-LMSNs) were prepared by hot water- film hydration method, and the characterized its morphology, particle size and release in vitro.  Meanwhile, the intracellular uptake and cell toxicity of CPT-11-LMSNs and intracellular accumulation of CPT-11 were evaluated on human breast carcinoma cell line (MCF-7).  The results indicated that the mean diameter of the spherical LMSNs was (120.27 ± 5.91) nm.  The slow release in simulated normal physiological conditions and a rapid release under simulated intracellular condition demonstrated the pH sensitivity of CPT-11-MSNs in vitro.  Moreover, the CPT-11-LMSN could improve the intracellular CPT-11 cumulant 2.1 times and reduce half maximal inhibitory concentration (IC50) values of CPT-11 1.4 times compared with CPT-11-MSNs, demonstrating a stronger cell lethality.

     

    • HTML全文
    • 参考文献(0)
    • 相关文章
    • 施引文献
  • 资源附件(0)

/

返回文章
返回