Structural modifications of 99mTc-labelled bombesin-like peptides for optimizing pharmacokinetics in prostate tumor targeting

dc.contributor.author	Λιόλιος, Χρήστος	el
dc.contributor.author	Φραγκογεώργη, Ειρήνη Α.	el
dc.contributor.author	Ζήκος, Χρήστος	el
dc.contributor.author	Λούντος, Γεώργιος	el
dc.contributor.author	Ξανθόπουλος, Σταύρος	el
dc.date.accessioned	2015-05-24T09:44:33Z
dc.date.available	2015-05-24T09:44:33Z
dc.date.issued	2015-05-24
dc.identifier.uri	http://hdl.handle.net/11400/11029
dc.rights	Αναφορά Δημιουργού-Μη Εμπορική Χρήση-Όχι Παράγωγα Έργα 3.0 Ηνωμένες Πολιτείες	*
dc.rights.uri	http://creativecommons.org/licenses/by-nc-nd/3.0/us/	*
dc.source	http://www.sciencedirect.com/science/article/pii/S0378517312001998	en
dc.subject	Pharmacokinetics
dc.subject	Scintigraphy
dc.subject	Φαρμακοκινητική
dc.subject	Σπινθηρογράφημα
dc.title	Structural modifications of 99mTc-labelled bombesin-like peptides for optimizing pharmacokinetics in prostate tumor targeting	en
heal.type	journalArticle
heal.classification	Technology
heal.classification	Biomedical engineering
heal.classification	Τεχνολογία
heal.classification	Βιοϊατρική τεχνολογία
heal.classificationURI	http://zbw.eu/stw/descriptor/10470-6
heal.classificationURI	http://id.loc.gov/authorities/subjects/sh85014237
heal.classificationURI	N/A-Τεχνολογία
heal.classificationURI	N/A-Βιοϊατρική τεχνολογία
heal.keywordURI	http://id.loc.gov/authorities/subjects/sh00006940
heal.keywordURI	http://lod.nal.usda.gov/148538
heal.contributorName	Μπουζιώτη, Πηνελόπη	el
heal.contributorName	Παραβάτου-Πετσώτα, Μαρία	el
heal.contributorName	Λιβανίου, Ευαγγελία	el
heal.contributorName	Βαρβαρήγου, Αλεξάνδρα Δ.	el
heal.contributorName	Sivolapenko, Gregory B.	en
heal.identifier.secondary	doi:10.1016/j.ijpharm.2012.02.049
heal.language	en
heal.access	campus
heal.recordProvider	Τ.Ε.Ι. Αθήνας. Σχολή Τεχνολογικών Εφαρμογών. Τμήμα Μηχανικών Βιοϊατρικής Τεχνολογίας Τ.Ε.	el
heal.publicationDate	2012
heal.bibliographicCitation	Liolios, C., Fragogeorgi, E., Zikos, C., Loudos, G., Xanthopoulos, S., et al. (July 2012). Structural modifications of 99mTc-labelled bombesin-like peptides for optimizing pharmacokinetics in prostate tumor targeting. International Journal of Pharmaceutics. 430(1-2). pp. 1-17. Elsevier B.V: 2012. Available from: http://www.sciencedirect.com/science/article/pii/S0378517312001998 [Accessed 10/03/2012]	en
heal.abstract	Purpose: The main goal of the present study was to investigate the importance of the addition of a positively charged aa in the naturally occurring Bombesin (BN) peptide for its utilization as radiodiagnostic agent, taking into consideration the biodistribution profile, the pharmacokinetic characteristics and the tumor targeting ability. Methods: Two BN-derivatives of the general structure [M-chelator]-(spacer)-BN(2–14)-NH2, where M: 99mTc or 185/187Re, chelator: Gly-Gly-Cys-, spacer: -(arginine)3-, M-BN-A; spacer: -(ornithine)3-, M-BN-O; have been prepared and evaluated as tumor imaging agents. Results: The peptides under study presented high radiolabelling efficiency (>98%), significant stability in human plasma (>60% intact radiolabelled peptide after 1 h incubation) and comparable receptor binding affinity with the standard [125I-Tyr4]-BN. Their internalization rates in the prostate cancer PC-3 cells differed, although the amount of internalized peptide was the same. The biodistribution and the dynamic -camera imaging studies in normal and PC-3 tumor-bearing SCID mice have shown significant tumor uptake, combined with fast blood clearance, through the urinary pathway. Conclusion: The addition of the charged aa spacer in the BN structure was advantageous for biodistribution, pharmacokinetics and tumor targeting ability, because it reduced the upper abdominal radioactivity levels and increased tumor/normal tissue contrast ratios.	en
heal.publisher	Elsevier B.V.	en
heal.journalName	International Journal of Pharmaceutics	en
heal.journalType	peer-reviewed
heal.fullTextAvailability	true