当前位置：
X-MOL 学术
›
Chem. Bio. Drug Des.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Design and fabrication of dual-targeted delivery system based on gemcitabine-conjugated human serum albumin nanoparticles.
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-06-22 , DOI: 10.1111/cbdd.13044 Parisa Norouzi 1 , Mohsen Amini 2 , Fatemeh Mottaghitalab 3 , Farnaz Sadat Mirzazadeh Tekie 3 , Rassoul Dinarvand 3 , Zahra Hadavand Mirzaie 3 , Fatemeh Atyabi 1, 3
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-06-22 , DOI: 10.1111/cbdd.13044 Parisa Norouzi 1 , Mohsen Amini 2 , Fatemeh Mottaghitalab 3 , Farnaz Sadat Mirzazadeh Tekie 3 , Rassoul Dinarvand 3 , Zahra Hadavand Mirzaie 3 , Fatemeh Atyabi 1, 3
Affiliation
|
Dual‐targeted drug delivery system has established their reputation as potent vehicles for cancer chemotherapies. Herein, gemcitabine (Gem) was conjugated to human serum albumin (HSA) via dithiodipropionic anhydride to fabricate Gem‐HSA nanoparticles. It was hypothesized that this system can enhance the low stability of Gem and can improve its intracellular delivery. Furthermore, folate was applied as targeting agent on HSA nanoparticles for increasing the tumor selectivity of Gem. To evaluate the structural properties of synthesized products, 1H NMR and FT‐IR were performed. Moreover, HPLC was implemented for confirming the conjugation between HSA and Gem. Nanoparticles have shown spherical shape with negative charge. The release rate of Gem was dependent to the concentration of glutathione and pH. Folate‐targeted HSA nanoparticles have shown higher cytotoxicity, cellular uptake, and apoptosis induction on folate receptor overexpressing MDA‐MB‐231 cells in comparison to non‐targeted nanoparticles. Finally, it is considered that the developed dual‐targeted nanoparticles would be potent in improving the stability and efficacy of intracellular delivery of Gem and its selective delivery to cancer cells.
中文翻译：
基于吉西他滨缀合的人血清白蛋白纳米粒子的双靶递送系统的设计和制造。
双目标药物递送系统已确立了其作为癌症化学疗法有效载体的声誉。在本文中，吉西他滨（Gem）通过二硫代二丙酸酐与人血清白蛋白（HSA）结合以制造Gem-HSA纳米粒子。据推测，该系统可以增强宝石的低稳定性，并可以改善其细胞内传递。此外，叶酸被用作HSA纳米颗粒上的靶向剂，以增加Gem的肿瘤选择性。要评估合成产品的结构特性，1进行1 H NMR和FT‐IR分析。此外，实施了HPLC以确认HSA与宝石之间的缀合。纳米颗粒显示带有负电荷的球形。宝石的释放速率取决于谷胱甘肽的浓度和pH。与非靶向纳米颗粒相比，以叶酸靶向的HSA纳米颗粒对过表达叶酸受体的MDA-MB-231细胞表现出更高的细胞毒性，细胞摄取和凋亡诱导作用。最后，可以认为，开发的双靶纳米粒子将有效提高Gem的细胞内传递及其向癌细胞的选择性传递的稳定性和功效。
更新日期：2017-06-22
中文翻译：
基于吉西他滨缀合的人血清白蛋白纳米粒子的双靶递送系统的设计和制造。
双目标药物递送系统已确立了其作为癌症化学疗法有效载体的声誉。在本文中，吉西他滨（Gem）通过二硫代二丙酸酐与人血清白蛋白（HSA）结合以制造Gem-HSA纳米粒子。据推测，该系统可以增强宝石的低稳定性，并可以改善其细胞内传递。此外，叶酸被用作HSA纳米颗粒上的靶向剂，以增加Gem的肿瘤选择性。要评估合成产品的结构特性，1进行1 H NMR和FT‐IR分析。此外，实施了HPLC以确认HSA与宝石之间的缀合。纳米颗粒显示带有负电荷的球形。宝石的释放速率取决于谷胱甘肽的浓度和pH。与非靶向纳米颗粒相比，以叶酸靶向的HSA纳米颗粒对过表达叶酸受体的MDA-MB-231细胞表现出更高的细胞毒性，细胞摄取和凋亡诱导作用。最后，可以认为，开发的双靶纳米粒子将有效提高Gem的细胞内传递及其向癌细胞的选择性传递的稳定性和功效。
京公网安备 11010802027423号