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dc.contributor.authorAccardo, Antonella
dc.contributor.authorSalsano, Giuseppina
dc.contributor.authorMorisco, Anna
dc.contributor.authorAurilio, Michela
dc.contributor.authorParisi, Antonio
dc.contributor.authorMaione, Francesco
dc.contributor.authorCicala, Carla
dc.contributor.authorTesauro, Diego
dc.contributor.authorAloj, Luigi
dc.contributor.authorDe Rosa, Giuseppe
dc.contributor.authorMorelli, Giancarlo
dc.date.accessioned2018-12-22T00:31:49Z
dc.date.available2018-12-22T00:31:49Z
dc.date.issued2012
dc.identifier.issn1176-9114
dc.identifier.urihttps://www.repository.cam.ac.uk/handle/1810/287418
dc.description.abstractOBJECTIVES: Drug delivery systems consisting of liposomes displaying a cell surface receptor-targeting peptide are being developed to specifically deliver chemotherapeutic drugs to tumors overexpressing a target receptor. This study addresses novel liposome composition approaches to specifically target tissues overexpressing bombesin (BN) receptors. METHODS: A new amphiphilic peptide derivative (MonY-BN) containing the BN(7-14) peptide, the DTPA (diethylenetriaminepentaacetate) chelating agent, a hydrophobic moiety with two C(18) alkyl chains, and polyethylene glycol spacers, has been synthesized by solid-phase methods. Liposomes have been generated by co-aggregation of MonY-BN with 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC). The structural and biological properties of these new target-selective drug-delivery systems have been characterized. RESULTS: Liposomes with a DSPC/MonY-BN (97/3 molar ratio) composition showed a diameter of 145.5 ± 31.5 nm and a polydispersity index of 0.20 ± 0.05. High doxorubicin (Dox) loading was obtained with the remote pH gradient method using citrate as the inner buffer. Specific binding to PC-3 cells of DSPC/MonY-BN liposomes was obtained (2.7% ± 0.3%, at 37°C), compared with peptide-free DSPC liposomes (1.4% ± 0.2% at 37°C). Incubation of cells with DSPC/ MonY-BN/Dox showed significantly lower cell survival compared with DSPC/Dox-treated cells, in the presence of 100 ng/mL and 300 ng/mL drug amounts, in cytotoxicity experiments. Intravenous treatment of PC-3 xenograft-bearing mice with DSPC/MonY-BN/Dox at 10 mg/kg Dox dose produced higher tumour growth inhibition (60%) compared with nonspecific DSPC/ Dox liposomes (36%) relative to control animals. CONCLUSION: The structural and loading properties of DSPC/MonY-BN liposomes along with the observed in-vitro and in-vivo activity are encouraging for further development of this approach for target-specific cancer chemotherapy.
dc.format.mediumPrint-Electronic
dc.languageeng
dc.publisherInforma UK Limited
dc.rightsPublisher's own licence
dc.subjectCell Line, Tumor
dc.subjectAnimals
dc.subjectMice, Inbred BALB C
dc.subjectHumans
dc.subjectMice
dc.subjectMice, Nude
dc.subjectProstatic Neoplasms
dc.subjectPentetic Acid
dc.subjectDoxorubicin
dc.subjectBombesin
dc.subjectPhosphatidylcholines
dc.subjectPeptide Fragments
dc.subjectReceptors, Bombesin
dc.subjectAntineoplastic Agents
dc.subjectLiposomes
dc.subjectDrug Carriers
dc.subjectSurface-Active Agents
dc.subjectDrug Delivery Systems
dc.subjectXenograft Model Antitumor Assays
dc.subjectFemale
dc.subjectMale
dc.subjectNanomedicine
dc.titlePeptide-modified liposomes for selective targeting of bombesin receptors overexpressed by cancer cells: a potential theranostic agent.
dc.typeArticle
prism.endingPage2017
prism.publicationDate2012
prism.publicationNameInt J Nanomedicine
prism.startingPage2007
prism.volume7
dc.identifier.doi10.17863/CAM.34722
rioxxterms.versionofrecord10.2147/IJN.S29242
rioxxterms.versionVoR
rioxxterms.licenseref.urihttp://www.rioxx.net/licenses/all-rights-reserved
rioxxterms.licenseref.startdate2012-01
dc.contributor.orcidAloj, Luigi [0000-0002-7452-4961]
dc.identifier.eissn1178-2013
rioxxterms.typeJournal Article/Review
cam.issuedOnline2012-04-17


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