title: Target selective micelles for bombesin receptors incorporating Au(III)-dithiocarbamato complexes.
abstract: Pure sterically stabilized micelles (SSM) of DSPE-PEG2000, and sterically stabilized mixed micelles (SSMM) containing PC or DOPC phospholipids (5, 10 or 20% mol/mol with respect to DSPE-PEG2000) are developed as delivery systems for the gold based cytotoxic drug Au(III)-dithiocarbamato complex AuL12. In particular, SSMM containing 5% of PC at 5mM of lipid concentration encapsulates 61.0 μg of AuL12 with a DL% of 1.13. The gold complex remains stable up to 72 h when incorporated in the aggregate, as indicated by UV-vis measurements. Incorporation in micelle composition of a low amount of the peptide derivative MonY-BN-AA1, containing a bombesin peptide analogue does not influence structural parameters of the micelles (diameter around 20 nm) neither the AuL12 loading parameters. Target selective properties of the peptide containing full aggregate on PC-3 cells overexpressing the GRP/bombesin receptors are observed by in vitro cytotoxic studies: a decrease of cell viability, ∼ 50%, is obtained in cells treated with AuL12-targeted micelles at 10 μM drug concentration for 48 h with respect to untargeted micelles.
authors.affiliation: University of Naples "Federico II", Department of Pharmacy, CIRPeB & IBB CNR, Via Mezzocannone 16, 80134 Napoli, Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Ringhieri
authors.affiliation: University of Naples "Federico II", Department of Pharmacy, CIRPeB & IBB CNR, Via Mezzocannone 16, 80134 Napoli, Italy.
authors.forename: Roberta
authors.initials: R
authors.lastname: Iannitti
authors.affiliation: University of Padua, Department of Chemical Sciences, Via Marzolo 1, 35131 Padova, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Nardon
authors.affiliation: University of Naples "Federico II", Department of Pharmacy, CIRPeB & IBB CNR, Via Mezzocannone 16, 80134 Napoli, Italy.
authors.forename: Rosanna
authors.initials: R
authors.lastname: Palumbo
authors.affiliation: University of Padua, Department of Chemical Sciences, Via Marzolo 1, 35131 Padova, Italy.
authors.forename: Dolores
authors.initials: D
authors.lastname: Fregona
authors.affiliation: University of Naples "Federico II", Department of Pharmacy, CIRPeB & IBB CNR, Via Mezzocannone 16, 80134 Napoli, Italy.
authors.forename: Giancarlo
authors.initials: G
authors.lastname: Morelli
authors.affiliation: University of Naples "Federico II", Department of Pharmacy, CIRPeB & IBB CNR, Via Mezzocannone 16, 80134 Napoli, Italy. Electronic address: antonella.accardo@unina.it.
authors.forename: Antonella
authors.initials: A
authors.lastname: Accardo
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D001839:Bombesin / Q000031:analogs & derivatives / Q000737:chemistry; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002945:Cisplatin / Q000737:chemistry* / Q000494:pharmacology; D056831:Coordination Complexes / Q000737:chemistry* / Q000494:pharmacology; D006046:Gold / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008823:Micelles; D010446:Peptide Fragments / Q000737:chemistry; D010713:Phosphatidylcholines / Q000737:chemistry; D010714:Phosphatidylethanolamines / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D018004:Receptors, Bombesin / Q000378:metabolism*
chemical_list: C519184:1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 2000); D000970:Antineoplastic Agents; D056831:Coordination Complexes; D008823:Micelles; D010446:Peptide Fragments; D010713:Phosphatidylcholines; D010714:Phosphatidylethanolamines; D018004:Receptors, Bombesin; C118536:bombesin (7-14); D011092:Polyethylene Glycols; D006046:Gold; C017251:1,2-oleoylphosphatidylcholine; D001839:Bombesin; D002945:Cisplatin
keywords: Bombesin peptide; Drug delivery; Gold complexes; Sterically stabilized micelles