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首页> 外文期刊>RSC Advances >Novel naproxen-peptide-conjugated amphiphilic dendrimer self-assembly micelles for targeting drug delivery to osteosarcoma cells
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Novel naproxen-peptide-conjugated amphiphilic dendrimer self-assembly micelles for targeting drug delivery to osteosarcoma cells

机译：用于靶向骨肉瘤细胞的新型萘普克伦 - 肽 - 缀合的两亲性树枝状胶片自组装胶束

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摘要

The aim of the current study was to synthesize and prepare novel self-assembly micelles loaded with curcumin (Cur) based on naproxen (Nap)-conjugated amphiphilic dendrimers. The apoptosis-inducing capacity of Nap-conjugated dendrimers and curcumin, the efficiency of uptake and the potential molecular mechanism on human osteosarcoma cells were investigated. The Nap-conjugated amphiphilic dendrimers were successfully synthesized, and the corresponding Cur-loaded micelles were conventionally prepared via self-assembly. These micelles showed good drug-encapsulating capacity, physiochemical properties, and drug-release profiles. The cellular proliferation and uptake assay suggested that the Cur-M-Nap induced more apoptosis of MG-63 human osteosarcoma cells. The western blot results suggested that these Nap-modified micelles could enhance the Cur-inducing apoptosis, mainly via intrinsic pathways and inhibition of the inflammation pathway. In summary, the Cur-loaded amphiphilic dendrimer-based micelles were successfully developed and they enhanced drug delivery to MG-63 cells. Mechanistic experiments suggested that Cur loaded into amphiphilic dendrimerbased micelles had a higher proliferation-inhibiting ability than free Cur, and could induce more apoptosis.
机译：目前研究的目的是合成和制备姜黄素（CUR）的新型自组装胶束，基于萘普生（午睡） - 缀合的两亲性树枝状晶夹。研究了嵌入式缀合的树枝状大分子和姜黄素的凋亡诱导能力，吸收效率和人骨肉瘤细胞上的潜在分子机制。成功地合成了嵌腔缀合的两亲性树枝状体，并且通常通过自组装制备相应的Cur-Loaded Micelles。这些胶束显示出良好的药物包封能力，物理化学性能和药物释放曲线。细胞增殖和摄取测定表明，Cur-M-Nap诱导Mg-63人骨瘤细胞的细胞凋亡。 Western印迹结果表明，这些露珠改性胶束可以增强Cur诱导的细胞凋亡，主要通过内在途径和炎症途径的抑制来增强。总之，成功地开发了加载的加载两亲性树枝状细胺胶束，并增强了药物递送至Mg-63细胞。机械实验表明，装载到两亲性树枝状胶束中的Cur具有比自由Cur的增殖抑制能力较高，并且可以诱导更多细胞凋亡。

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  • 来源
    《RSC Advances》 |2016年第65期|共9页
  • 作者

    Zhao Yinbo; Zeng Qi; Wu Fengbo; Li Jing; Pan Zhaoping; Shen Pengfei; Yang Lu; Xu Ting; Cai Lulu; Guo Li;

  • 作者单位

    Sichuan Univ West China Sch Pharm Dept Med Chem Key Lab Drug Targeting &

    Drug Delivery Syst Minis Chengdu 610041 Peoples R China;

    Sichuan Univ West China Med Sch West China Hosp Dept Pharm Chengdu 610041 Peoples R China;

    Sichuan Univ West China Sch Pharm Dept Med Chem Key Lab Drug Targeting &

    Drug Delivery Syst Minis Chengdu 610041 Peoples R China;

    Sichuan Univ West China Med Sch West China Hosp Dept Pharm Chengdu 610041 Peoples R China;

    Sichuan Univ West China Sch Pharm Dept Med Chem Key Lab Drug Targeting &

    Drug Delivery Syst Minis Chengdu 610041 Peoples R China;

    Sichuan Univ West China Med Sch West China Hosp Dept Pharm Chengdu 610041 Peoples R China;

    Sichuan Univ West China Med Sch West China Hosp Dept Pharm Chengdu 610041 Peoples R China;

    Sichuan Univ West China Med Sch West China Hosp Dept Pharm Chengdu 610041 Peoples R China;

    Hosp Univ Elect Sci &

    Technol China Personalized Drug Therapy Key Lab Sichuan Prov Chengdu 610072 Peoples R China;

    Sichuan Univ West China Sch Pharm Dept Med Chem Key Lab Drug Targeting &

    Drug Delivery Syst Minis Chengdu 610041 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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