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New Peptide Functionalized Nanostructured Lipid Carriers with CNS Drugs and Evaluation Anti-proliferative Activity

2022-06-26Journal article Open access
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dc.contributor.authorSilva, Sara
dc.contributor.authorMarto, Joana
dc.contributor.authorGonçalves, Lídia
dc.contributor.authorDuarte, Diana
dc.contributor.authorSoares, Olívia Salomé G. P.
dc.contributor.authorVasques-Nóvoa, Francisco
dc.contributor.authorAlmeida, António J.
dc.contributor.authorVale, Nuno
dc.date.accessioned2022-08-09T19:02:31Z
dc.date.available2022-08-09T19:02:31Z
dc.date.issued2022-06-26
dc.date.updated2022-06-29T14:53:07Z
dc.description.abstractNanoparticulate systems have been widely investigated as delivery vectors for efficient drug delivery in different diseases. Nanostructured lipid carriers (NLC) are composed of both solid and liquid lipids (glyceryl dibehenate and diethylene glycol monoethyl ether) and have demonstrated enhanced biological compatibility and increased drug loading capability. Furthermore, the use of peptides, in particular cell-penetrating peptides, to functionalize nanoparticles and enhance cell membrane permeation was explored in this paper. In this paper, we described the synthesis of a new conjugated of tranylcypromine with MAP. In addition, taking into consideration our previous results, this study developed different NLCs loaded with three central nervous system (CNS) drugs (tacrine (TAC), rasagiline (RAS), and tranylcypromine (TCP)) functionalized with model amphipathic peptide (MAP) and evaluated their activity against cancer cells. Particle size analysis demonstrated NLC presented less than 200 nm and a polydispersity index less than 0.3. Moreover, in vitro results showed that conjugation of MAP with drugs led to a higher decrease in cell viability of a neuroblastoma cell line and Caco-2 cell line, more than MAP alone. Furthermore, NLC encapsulation contributed to higher cellular delivery and enhanced toxic activity at lower concentrations when compared with free or co-administration drug-MAP conjugate.pt_PT
dc.description.sponsorshipFunding: This work was financed by FEDER—Fundo Europeu de Desenvolimento Regional through the COMPETE 2020—Operational Programme for Competitiveness and Internationalization (POCI), Portugal 2020, and by Portuguese funds through FCT—Fundação para a Ciência e a Tecnologia, in a framework of the projects in CINTESIS, R&D Unit (reference UIDB/4255/2020, RISE (RISELA/P/0053/2020) and iMed.ULisboa (UID/DTP/04138/2019), as well by LA/P/0045/2020 (ALiCE), UIDB/50020/2020 and UIDP/50020/2020 (LSRE-LCM), funded by national funds through FCT/MCTES (PIDDAC). N.V. also thanks support from FCT and FEDER (European Union), award number IF/00092/2014/CP1255/CT0004 and CHAIR in Onco-Innovation. Acknowledgments: N.V. thanks support FCT and FEDER (European Union), award number IF/00092/ 2014/CP1255/CT0004 and CHAIR in Onco-Innovation. S.S. thanks FCT for PhD Grant (PD/BD/135456/ 2017) and PhD Programme in Medicines and Pharmaceutical Innovation (i3DU) from the University of Lisbon (Portugal) and the University of Porto (Portugal). D.D. acknowledges FCT for funding her PhD grant (SFRH/BD/140734/2018).pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationSilva S, Marto J, Gonçalves LM, Duarte D, Soares OSGP, Vasques-Nóvoa F, et al. New Peptide Functionalized Nanostructured Lipid Carriers with CNS Drugs and Evaluation Anti-proliferative Activity. IJMS 2022;23:7109. https://doi.org/10.3390/ijms23137109.pt_PT
dc.identifier.doi10.3390/ijms23137109pt_PT
dc.identifier.issn1422-0067
dc.identifier.slugcv-prod-3015150
dc.identifier.urihttp://hdl.handle.net/10451/54100
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherMDPIpt_PT
dc.relationUIDB/4255/2020pt_PT
dc.relationRISELA/P/0053/2020pt_PT
dc.relationResearch Institute for Medicines
dc.relationLaboratory of Separation and Reaction Engineering - Laboratory of Catalysis and Materials
dc.relationLaboratory of Separation and Reaction Engineering - Laboratory of Catalysis and Materials
dc.relationNew advance in biomedicine: peptide-mediated target drug delivery
dc.relationDesenvolvimento de um novo modelo de combinação de fármacos para o combate do cancro
dc.relation.publisherversionhttps://www.mdpi.com/1422-0067/23/13/7109pt_PT
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.subjectLipid nanoparticlespt_PT
dc.subjectCancer cell linespt_PT
dc.subjectCell-penetrating peptidespt_PT
dc.subjectDrug repurposingpt_PT
dc.subjectCytotoxicity assayspt_PT
dc.titleNew Peptide Functionalized Nanostructured Lipid Carriers with CNS Drugs and Evaluation Anti-proliferative Activitypt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleResearch Institute for Medicines
oaire.awardTitleLaboratory of Separation and Reaction Engineering - Laboratory of Catalysis and Materials
oaire.awardTitleLaboratory of Separation and Reaction Engineering - Laboratory of Catalysis and Materials
oaire.awardTitleNew advance in biomedicine: peptide-mediated target drug delivery
oaire.awardTitleDesenvolvimento de um novo modelo de combinação de fármacos para o combate do cancro
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FDTP%2F04138%2F2019/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F50020%2F2020/PT
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oaire.awardURIinfo:eu-repo/grantAgreement/FCT/POR_NORTE/SFRH%2FBD%2F140734%2F2018/PT
oaire.citation.conferencePlaceSwitzerlandpt_PT
oaire.citation.issue13pt_PT
oaire.citation.startPage7109pt_PT
oaire.citation.titleInternational Journal of Molecular Sciencespt_PT
oaire.citation.volume23pt_PT
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person.familyNameSilva
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person.familyNameSousa Duarte
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person.givenNameLídia Maria
person.givenNameDiana
person.givenNameSalomé
person.givenNameFrancisco
person.givenNameAntónio José
person.givenNameNuno
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