Han Yiqun, Li Ye, Zhang Peng, Sun Jiping, Li Xianzhen, Sun Xin, Kong Fansheng
a Department of Respiratory Medicine , General Hospital of Ji'nan Command , Ji'nan , People's Republic of China .
b Center of Interventional Therapy, Ji'nan Infectious Disease Hospital , Ji'nan , People's Republic of China , and.
Pharm Dev Technol. 2016;21(3):277-81. doi: 10.3109/10837450.2014.996900. Epub 2015 Jan 5.
Nanostructured lipid carriers (NLC) are potentially good colloidal drug carriers for gene delivery. They are advised to be the second lifetime of lipid nanocarriers.
The aim of this study is to develop novel modified NLC as nanomedicine for delivery of plasmid-containing enhanced green fluorescence protein (pEGFP). This system could target the lung cancer cells through receptor-mediated pathways to increase the nuclear uptake of genetic materials.
In the present study, pEGFP-loaded NLC (NLC/pEGFP) were prepared. Transferrin (Tf) containing ligands were used for the surface coating of the vectors. In vitro transfection efficiency of the modified vectors was evaluated in human alveolar adenocarcinoma cell line (A549 cells) and in vivo transfection efficiency of the modified vectors was evaluated on mice bearing A549 cells model.
Tf-modified NLC/pEGFP (Tf-NLC/pEGFP) has a particle size of 157 nm, and ∼ 82% of gene loading quantity. Tf-NLC/pEGFP displayed remarkably higher transfection efficiency than non-modified NLC/pEGFP both in vitro and in vivo.
The results demonstrate that the novel NLC gene delivery system offers an effective strategy for lung cancer gene therapy.
纳米结构脂质载体(NLC)是用于基因递送的潜在优良胶体药物载体。它们被认为是脂质纳米载体的第二代。
本研究旨在开发新型修饰的NLC作为纳米药物,用于递送含增强型绿色荧光蛋白(pEGFP)的质粒。该系统可通过受体介导的途径靶向肺癌细胞,以增加遗传物质的核摄取。
在本研究中,制备了负载pEGFP的NLC(NLC/pEGFP)。含转铁蛋白(Tf)的配体用于载体的表面包被。在人肺泡腺癌细胞系(A549细胞)中评估修饰载体的体外转染效率,并在荷A549细胞模型的小鼠上评估修饰载体的体内转染效率。
Tf修饰的NLC/pEGFP(Tf-NLC/pEGFP)粒径为157nm,基因负载量约为82%。Tf-NLC/pEGFP在体外和体内均显示出比未修饰的NLC/pEGFP显著更高的转染效率。
结果表明,新型NLC基因递送系统为肺癌基因治疗提供了一种有效的策略。