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Formulation, characterization, and cytotoxicity evaluation of lactoferrin functionalized lipid nanoparticles for riluzole delivery to the brain

2022-01-13Journal article Open access
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dc.contributor.authorTeixeira, Maria Inês
dc.contributor.authorLopes, Carla Martins
dc.contributor.authorGonçalves, Hugo
dc.contributor.authorCatita, José
dc.contributor.authorSilva, Ana Margarida
dc.contributor.authorRodrigues, Francisca
dc.contributor.authorAmaral, Maria Helena
dc.contributor.authorCosta, Paulo C.
dc.date.accessioned2022-01-19T12:40:54Z
dc.date.available2022-01-19T12:40:54Z
dc.date.issued2022-01-13
dc.description.abstractAmyotrophic lateral sclerosis (ALS) is a neurodegenerative disease with a very poor prognosis. Its treatment is hindered by a lack of new therapeutic alternatives and the existence of the blood–brain barrier (BBB), which restricts the access of drugs commonly used in ALS, such as riluzole, to the brain. To overcome these limitations and increase brain targeting, riluzole-loaded nanostructured lipid carriers (NLC) were prepared and functionalized with lactoferrin (Lf), facilitating transport across the BBB by interacting with Lf receptors expressed in the brain endothelium. NLC were characterized with respect to their physicochemical properties (size, zeta potential, polydispersity index) as well as their stability, encapsulation efficiency, morphology, in vitro release profile, and biocompatibility. Moreover, crystallinity and melting behavior were assessed by DSC and PXRD. Nanoparticles exhibited initial mean diameters between 180 and 220 nm and a polydispersity index below 0.3, indicating a narrow size distribution. NLC remained stable over at least 3 months. Riluzole encapsulation efficiency was very high, around 94–98%. FTIR and protein quantification studies confirmed the conjugation of Lf on the surface of the nanocarriers, with TEM images showing that the functionalized NLC presented a smooth surface and uniform spherical shape. An MTT assay revealed that the nanocarriers developed in this study did not cause a substantial reduction in the viability of NSC-34 and hCMEC/D3 cells at a riluzole concentration up to 10 μM, being therefore biocompatible. The results suggest that Lf-functionalized NLC are a suitable and promising delivery system to target riluzole to the brain.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationTeixeira, M.I.; Lopes, C.M.; Gonçalves, H.; Catita, J.; Silva, A.M.; Rodrigues, F.; Amaral, M.H.; Costa, P.C. Formulation, Characterization, and Cytotoxicity Evaluation of Lactoferrin Functionalized Lipid Nanoparticles for Riluzole Delivery to the Brain. Pharmaceutics 2022, 14, 185. https://doi.org/10.3390/ pharmaceutics14010185pt_PT
dc.identifier.doi10.3390/pharmaceutics14010185pt_PT
dc.identifier.issn1999-4923
dc.identifier.urihttp://hdl.handle.net/10284/10656
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherMDPIpt_PT
dc.relationThis work was financed by national funds from FCT—Fundação para a Ciência e a Tecnologia, I.P., in the scope of the projects UIDP/04378/2020 and UIDB/04378/2020 of the Research Unit on Applied Molecular Biosciences—UCIBIOpt_PT
dc.subjectBlood–brain barrier (BBB)pt_PT
dc.subjectBrain deliverypt_PT
dc.subjectNeurodegenerative diseasespt_PT
dc.subjectAmyotrophic lateral sclerosis (ALS)pt_PT
dc.subjectLipid nanoparticlept_PT
dc.subjectNanostructured lipid carriers (NLC)pt_PT
dc.subjectRiluzolept_PT
dc.subjectLactoferrinpt_PT
dc.subjectLactoferrin receptorspt_PT
dc.subjectDrug targetingpt_PT
dc.titleFormulation, characterization, and cytotoxicity evaluation of lactoferrin functionalized lipid nanoparticles for riluzole delivery to the brainpt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.issue1pt_PT
oaire.citation.startPage185pt_PT
oaire.citation.titlePharmaceuticspt_PT
oaire.citation.volume14pt_PT
person.familyNameLopes
person.familyNameMorais Catita
person.givenNameCarla
person.givenNameJose Antonio
person.identifierJose Catita
person.identifier.ciencia-id901D-160C-633E
person.identifier.ciencia-idB41E-3287-E706
person.identifier.orcid0000-0001-5080-032X
person.identifier.orcid0000-0001-7270-5702
person.identifier.ridM-4689-2016
person.identifier.scopus-author-id26649517700
person.identifier.scopus-author-id6507275921
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublicationd2a48cfe-9258-4916-99be-bbcb710f6605
relation.isAuthorOfPublication24bb2971-32ae-429b-b397-145dacb66a5a
relation.isAuthorOfPublication.latestForDiscoveryd2a48cfe-9258-4916-99be-bbcb710f6605

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