Zhang Yin-Long, Zhang Zhen-Hai, Jiang Tian-Yue, Lv Hui-Xia, Zhou Jian-Ping
Department of Pharmaceutics, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, PR China.
Pharmazie. 2013 Jan;68(1):47-53.
The aim of this study was to investigate the cytotoxicity of paclitaxel solid lipid nanoparticles (SLN) modified with stearic acid octaarginine (SA-R8-PTX-SLN) as well as the cellular uptake of coumarin-6-loaded SLN modified with SA-R8 (SA-R8-C6-SLN) in human lung cancer cells, A549. SLN were prepared using a film dispersion method; and then their particle size, zeta potential, morphology, bound efficiency of SAR8, drug loading efficiency, and in vitro release were characterized. SA-R8-PTX-SLN and SA-R8-C6-SLN were incubated with A549 cells to measure their cytotoxicity and cellular uptake, respectively. The results indicated that the cytotoxicity of SA-R8-PTX-SLN was enhanced significantly with the increasing amount of SA-R8 and the cellular uptakes of SLN increased with the incubated concentrations and the incubated time of SLN. In contrast, SA-R8-SLN could significantly enhance the cellular uptake of SLN and the cytotoxicity of PTX in A549 cells. These in vitro results suggest that SA-R8-SLN could be proposed as alternative drug delivery system.
本研究旨在探讨硬脂酸八聚精氨酸修饰的紫杉醇固体脂质纳米粒(SA-R8-PTX-SLN)的细胞毒性,以及硬脂酸八聚精氨酸修饰的载香豆素-6固体脂质纳米粒(SA-R8-C6-SLN)在人肺癌细胞A549中的细胞摄取情况。采用薄膜分散法制备固体脂质纳米粒;然后对其粒径、zeta电位、形态、SA-R8结合效率、载药效率和体外释放进行表征。将SA-R8-PTX-SLN和SA-R8-C6-SLN分别与A549细胞孵育,以测定它们的细胞毒性和细胞摄取情况。结果表明,SA-R8-PTX-SLN的细胞毒性随着SA-R8含量的增加而显著增强,且固体脂质纳米粒的细胞摄取量随固体脂质纳米粒的孵育浓度和孵育时间增加。相比之下,SA-R8-SLN可显著增强A549细胞中固体脂质纳米粒的细胞摄取及紫杉醇的细胞毒性。这些体外实验结果表明,SA-R8-SLN可作为替代药物递送系统。