Cell uptake of paclitaxel solid lipid nanoparticles modified by cell-penetrating peptides in A549 cells

作者：Zhang, Yin-Long; Zhang, Zhen-Hai; Jiang, Tian-Yue; Ayman-Waddad; Jing-Li; Lv, Hui-Xia^*; Zhou, Jian-Ping

来源：Pharmazie, 2013, 68(1): 47-53.

DOI：10.1691/ph.2013.2071

• ARGININE-RICH PEPTIDES
• INTRACELLULAR DELIVERY
• DRUG-DELIVERY
• IN-VITRO
• CANCER-CELLS
• CYTOTOXICITY
• PHARMACOKINETICS
• MOLECULES
• LIPOSOMES
• POLYMERS

The aim of this study was to investigate the cytotoxicity of paclitaxel solid lipid nanoparticles (SLN) modified with stearic acid octaarginine (SA-R-8-PTX-SLN) as well as the cellular uptake of coumarin-6-loaded SLN modified with SA-R-8 (SA-R-8-C-6-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 SA-R-8, drug loading efficiency, and in vitro release were characterized. SA-R-8-PTX-SLN and SA-R-8-C-6-SLN were incubated with A549 cells to measure their cytotoxicity and cellular uptake, respectively. The results indicated that the cytotoxicity of SA-R-8-PTX-SLN was enhanced significantly with the increasing amount of SA-R-8 and the cellular uptakes of SLN increased with the incubated concentrations and the incubated time of SLN. In contrast, SA-R-8-SLN could significantly enhance the cellular uptake of SLN and the cytotoxicity of PTX in A549 cells. These in vitro results suggest that SA-R-8-SLN could be proposed as alternative drug delivery system.

• 出版日期2013-1
• 单位中国药科大学; 江苏省中医药研究院