title: Cell uptake of paclitaxel solid lipid nanoparticles modified by cell-penetrating peptides in A549 cells.
abstract: 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.
authors: Department of Pharmaceutics, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, PR China.
authors: Yin-Long
authors: YL
authors: Zhang
authors: Zhen-Hai
authors: ZH
authors: Zhang
authors: Tian-Yue
authors: TY
authors: Jiang
authors: Ayman-Waddad
authors: Jing-Li
authors: Hui-Xia
authors: HX
authors: Lv
authors: Jian-Ping
authors: JP
authors: Zhou
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003374:Coumarins / Q000493:pharmacokinetics; D003956:Dialysis; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008055:Lipids / Q000737:chemistry; D018625:Microscopy, Atomic Force; D008856:Microscopy, Fluorescence; D053758:Nanoparticles; D017239:Paclitaxel / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D010316:Particle Size; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D003374:Coumarins; D008055:Lipids; D010455:Peptides; C030123:coumarin; D017239:Paclitaxel