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Delivery as nanoparticles reduces imatinib mesylate-induced cardiotoxicity and improves anticancer activity

2015Journal article Open access
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dc.contributor.authorMarslin, Gregory
dc.contributor.authorRevina, Ann Mary
dc.contributor.authorKhandelwal, Vinoth Kumar Megraj
dc.contributor.authorBalakumar, Krishnamoorthy
dc.contributor.authorPrakash, Jose
dc.contributor.authorFranklin, Gregory
dc.contributor.authorSheeba, Caroline Jeya
dc.date.accessioned2018-12-07T14:58:26Z
dc.date.available2018-12-07T14:58:26Z
dc.date.issued2015
dc.description.abstractClinical effectiveness of imatinib mesylate in cancer treatment is compromised by its off-target cardiotoxicity. In the present study, we have developed physically stable imatinib mesylate-loaded poly(lactide-co-glycolide) nanoparticles (INPs) that could sustainably release the drug, and studied its efficacy by in vitro anticancer and in vivo cardiotoxicity assays. MTT (methylthiazolyldiphenyl-tetrazolium bromide) assay revealed that INPs are more cytotoxic to MCF-7 breast cancer cells compared to the equivalent concentration of free imatinib mesylate. Wistar rats orally administered with 50 mg/kg INPs for 28 days showed no significant cardiotoxicity or associated changes. Whereas, increased alanine aminotransferase, aspartate aminotransferase, and alkaline phosphatase levels, and reduced white blood cell, red blood cell, and hemoglobin content were observed in the animals administered with free drug. While the histological sections from hearts of animals that received INPs did not show any significant cardiotoxic symptoms, loss of normal architecture and increased cytoplasmic vacuolization were observed in the heart sections of animals administered with free imatinib mesylate. Based on these results, we conclude that nano-encapsulation of imatinib mesylate increases its efficacy against cancer cells, with almost no cardiotoxicity.
dc.identifier.doi10.2147/IJN.S75962
dc.identifier.issn1178-2013
dc.identifier.urihttp://hdl.handle.net/10400.1/12026
dc.language.isoeng
dc.peerreviewedyes
dc.publisherDove Medical Press
dc.relationSHEDDING LIGHT ON THE CONTROVERSY: ESTABLISHING THE EMBRYO MOLECULAR CLOCK AS AN INTEGRAL COMPONENT OF THE LIMB PATTERNING MACHINERY
dc.subjectTyrosine kinase nhibitor
dc.subjectBcr-abl
dc.subjectPolymeric nanoparticles
dc.subjectAntitumor-activity
dc.subjectDoxorubicin
dc.subjectToxicity
dc.subjectGrowth
dc.subjectCells
dc.subjectCombination
dc.subjectTherapy
dc.titleDelivery as nanoparticles reduces imatinib mesylate-induced cardiotoxicity and improves anticancer activity
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleSHEDDING LIGHT ON THE CONTROVERSY: ESTABLISHING THE EMBRYO MOLECULAR CLOCK AS AN INTEGRAL COMPONENT OF THE LIMB PATTERNING MACHINERY
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBD%2F72809%2F2010/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT//SFRH%2FBPD%2F89493%2F2012/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/COMPETE/PTDC%2FAGR-GPL%2F119211%2F2010/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876/UID%2FAGR%2F04033%2F2013/PT
oaire.citation.endPage3170
oaire.citation.startPage3163
oaire.citation.titleInternational Journal of Nanomedicine
oaire.citation.volume10
oaire.fundingStreamSFRH
oaire.fundingStreamCOMPETE
oaire.fundingStream5876
person.familyNameSheeba
person.givenNameCaroline Jeya
person.identifier437977
person.identifier.orcid0000-0001-5357-4743
person.identifier.ridB-5177-2011
person.identifier.scopus-author-id6504257550
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccess
rcaap.typearticle
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