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Riluzole-loaded lipid nanoparticles for brain delivery: preparation, optimization and characterization

2023Journal article Restricted 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.accessioned2024-01-29T16:51:56Z
dc.date.available2024-01-29T16:51:56Z
dc.date.issued2023
dc.description.abstractAmyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease, with a median survival of only 2 to 4 years. Riluzole, a drug commonly used in the management of ALS, has a low aqueous solubility and limited bioavailability. ALS treatment is also hindered by the presence of the blood–brain barrier (BBB) that preserves the delicate homeostasis of the cerebral milieu, isolating it and making brain drug delivery exceptionally hard. To overcome these issues, the use of lipid nanocarriers, such as solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC), is a promising strategy. In this study, SLN and NLC were prepared and optimized to facilitate riluzole uptake into the brain for ALS therapy. The lipid nanoparticles were characterized through different techniques, with respect to their physicochemical properties (size, zeta potential (ZP), polydispersity index (PDI)), as well as encapsulation efficiency, morphology, stability, in vitro release, crystallinity, and biocompatibility. Riluzole-loaded nanocarriers exhibited characteristics suitable for brain delivery, including mean diameters between 147.2 and 203.1 nm, low PDI (<0.3), and negative ZP between − 22.5 and − 27.5 mV. Additionally, they were physically stable over 3 months under storage conditions (5 ℃ and 25 ℃), promoting a slow and sustained release of the drug, which was shown to be inside the core of the lipid matrix. Cytotoxicity assays demonstrated that both SLN and NLC did not significantly affect the viability of an hCMEC/D3 cell monolayer at a riluzole concentration up to 10 μM. The results suggest that the developed nanocarriers could be a viable platform to target riluzole to the central nervous system (CNS). Nevertheless, further in vitro and in vivo studies are needed to validate their therapeutic efficacy and safety.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationInês Teixeira, M., Lopes, C. M., Gonçalves, H., Catita, J., Margarida Silva, A., Rodrigues, F., Helena Amaral, M., & Costa, P. C. (2023). Riluzole-loaded lipid nanoparticles for brain delivery: preparation, optimization and characterization. Journal of Molecular Liquids, 122749. https://doi.org/10.1016/j.molliq.2023.122749pt_PT
dc.identifier.doi10.1016/j.molliq.2023.122749pt_PT
dc.identifier.issn0167-7322
dc.identifier.urihttp://hdl.handle.net/10284/12621
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherElsevierpt_PT
dc.subjectAmyotrophic lateral sclerosis (ALS)pt_PT
dc.subjectBrain deliverypt_PT
dc.subjectRiluzolept_PT
dc.subjectLipid nanoparticlespt_PT
dc.subjectSolid lipid nanoparticles (SLN)pt_PT
dc.subjectNanostructured lipid carriers (NLC)pt_PT
dc.titleRiluzole-loaded lipid nanoparticles for brain delivery: preparation, optimization and characterizationpt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.startPage122749pt_PT
oaire.citation.titleJournal of Molecular Liquidspt_PT
oaire.citation.volume388pt_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.rightsrestrictedAccesspt_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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