Antilung cancer effect of ergosterol and cisplatin-loaded liposomes modified with cyclic arginine-glycine-aspartic acid and octa-arginine peptides.
作者： Meijia Wu , Ting Huang , Juan Wang , Ping Chen , Wanwan Mi
DOI: 10.1097/MD.0000000000011916
关键词:
摘要: BACKGROUND Lung cancer is one of the most important diseases threatening human health, and targeted therapy has become main research direction. This work, therefore, aimed to develop cyclic arginine-glycine-aspartic (RGD) octa-arginine (R8) peptide-modified ergosterol (ERG)-combined cisplatin (diamminedichloridoplatinum(II) [DDP]) liposomes (LIP) as a drug delivery system. METHODS Soybean phospholipids (SPC) cholesterol (Chol) were selected prepare different LIPs: ERG-loaded LIP (ERG-LIP), DDP ERG-LIP (DDP/ERG-LIP), R8 (R8-DDP/ERG-LIP), RGD R8-DDP/ERG-LIP (RGD/R8-DDP/ERG-LIP). The quality, tumor sphere penetrating ability, in vitro cellular uptake, mechanism cytotoxicity RGD/R8-DDP/ERG-LIP evaluated. RESULTS quality evaluation revealed that round with double-layer structure. average particle size, dispersion coefficient polydispersity index (PDI), zeta potential 155.2 ± 8.7 nm, 0.102, 4.74 ± 0.7 mV, respectively. Furthermore, LIPs stable serum, obviously inhibited growth A549 lung cells exhibiting strongest inhibitory effect. highest uptake rate, which was at 4 hours, exhibited by concentration-dependent manner. CONCLUSION results showed mainly clathrin-mediated endocytosis pathway (chlorpromazine). also suggest might be promising system improve antilung effect tumor-targeting vitro.
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