Publication
Formulation, Characterization, and Cytotoxicity Evaluation of Lactoferrin Functionalized Lipid Nanoparticles for Riluzole Delivery to the Brain
dc.contributor.author | Teixeira, Maria Inês | |
dc.contributor.author | Lopes, Carla Martins | |
dc.contributor.author | Gonçalves, Hugo | |
dc.contributor.author | Catita, José | |
dc.contributor.author | Silva, Ana Margarida | |
dc.contributor.author | Rodrigues, Francisca | |
dc.contributor.author | Amaral, Maria Helena | |
dc.contributor.author | Costa, Paulo C. | |
dc.date.accessioned | 2023-01-31T09:17:35Z | |
dc.date.available | 2023-01-31T09:17:35Z | |
dc.date.issued | 2022-01-13 | |
dc.description.abstract | Amyotrophic 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.sponsorship | This 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—UCIBIO. Maria Inês Teixeira is thankful for the Ph.D. grant (2020.05060.BD) from the Fundação para a Ciência e a Tecnologia (FCT) and for project LA/P/0140/2020 of the Associate Laboratory Institute for Health and Bioeconomy—i4HB supported through national funds. Ana Margarida Silva is thankful for the Ph.D. grant (SFRH/BD/144994/2019) financed by POPH–QREN and subsidized by the European Science Foundation and Ministério da Ciência, Tecnologia e Ensino Superior. Francisca Rodrigues (CEECIND/01886/2020) is thankful for her contract financed by FCT/MCTES—CEEC Individual Program Contract and for projects UIDB/50006/2020 and UIDP/50006/2020 by the FCT/Ministério da Ciência, Tecnologia e Ensino Superior (MCTES) supported through national funds. The authors are also grateful to Rui Fernandes and Ana Rita Malheiro (HEMS core facility, i3S, University of Porto) for their assistance with TEM. | pt_PT |
dc.description.version | info:eu-repo/semantics/publishedVersion | pt_PT |
dc.identifier.doi | 10.3390/pharmaceutics14010185 | pt_PT |
dc.identifier.uri | http://hdl.handle.net/10400.22/22016 | |
dc.language.iso | eng | pt_PT |
dc.publisher | MDPI | pt_PT |
dc.relation | LA/P/0140/2020 | pt_PT |
dc.relation | Applied Molecular Biosciences Unit | |
dc.relation | Applied Molecular Biosciences Unit | |
dc.relation | Functionalized lipid nanocarriers for enhancement of blood-brain barrier BBB permeability in the treatment of amyotrophic lateral sclerosis | |
dc.relation | From soil to skin: Eco-friendly extract from kiwiberry leaves for prevention of skin aging process | |
dc.relation | Associated Laboratory for Green Chemistry - Clean Technologies and Processes | |
dc.relation | Associated Laboratory for Green Chemistry - Clean Technologies and Processes | |
dc.relation.publisherversion | https://www.mdpi.com/1999-4923/14/1/185 | pt_PT |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | pt_PT |
dc.subject | Blood–brain barrier (BBB) | pt_PT |
dc.subject | Brain delivery | pt_PT |
dc.subject | Neurodegenerative diseases | pt_PT |
dc.subject | Amyotrophic lateral sclerosis (ALS) | pt_PT |
dc.subject | Lipid nanoparticles | pt_PT |
dc.subject | Nanostructured lipid carriers (NLC) | pt_PT |
dc.subject | Riluzole | pt_PT |
dc.subject | Lactoferrin | pt_PT |
dc.subject | Lactoferrin receptors | pt_PT |
dc.subject | Drug targeting | pt_PT |
dc.title | Formulation, Characterization, and Cytotoxicity Evaluation of Lactoferrin Functionalized Lipid Nanoparticles for Riluzole Delivery to the Brain | pt_PT |
dc.type | journal article | |
dspace.entity.type | Publication | |
oaire.awardTitle | Applied Molecular Biosciences Unit | |
oaire.awardTitle | Applied Molecular Biosciences Unit | |
oaire.awardTitle | Functionalized lipid nanocarriers for enhancement of blood-brain barrier BBB permeability in the treatment of amyotrophic lateral sclerosis | |
oaire.awardTitle | From soil to skin: Eco-friendly extract from kiwiberry leaves for prevention of skin aging process | |
oaire.awardTitle | Associated Laboratory for Green Chemistry - Clean Technologies and Processes | |
oaire.awardTitle | Associated Laboratory for Green Chemistry - Clean Technologies and Processes | |
oaire.awardURI | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDP%2F04378%2F2020/PT | |
oaire.awardURI | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F04378%2F2020/PT | |
oaire.awardURI | info:eu-repo/grantAgreement/FCT//2020.05060.BD/PT | |
oaire.awardURI | info:eu-repo/grantAgreement/FCT/POR_NORTE/SFRH%2FBD%2F144994%2F2019/PT | |
oaire.awardURI | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F50006%2F2020/PT | |
oaire.awardURI | info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDP%2F50006%2F2020/PT | |
oaire.citation.issue | 1 | pt_PT |
oaire.citation.startPage | 185 | pt_PT |
oaire.citation.title | Pharmaceutics | pt_PT |
oaire.citation.volume | 14 | pt_PT |
oaire.fundingStream | 6817 - DCRRNI ID | |
oaire.fundingStream | 6817 - DCRRNI ID | |
oaire.fundingStream | POR_NORTE | |
oaire.fundingStream | 6817 - DCRRNI ID | |
oaire.fundingStream | 6817 - DCRRNI ID | |
person.familyName | Silva | |
person.familyName | Pinto Lisboa Martins Rodrigues Sarmento | |
person.givenName | Ana Margarida | |
person.givenName | Francisca | |
person.identifier | 1552042 | |
person.identifier.ciencia-id | 5C16-8C22-EF1E | |
person.identifier.ciencia-id | 4F19-3D98-2CBA | |
person.identifier.orcid | 0000-0002-1823-9816 | |
person.identifier.orcid | 0000-0001-8803-0041 | |
person.identifier.scopus-author-id | 57203495060 | |
project.funder.identifier | http://doi.org/10.13039/501100001871 | |
project.funder.identifier | http://doi.org/10.13039/501100001871 | |
project.funder.identifier | http://doi.org/10.13039/501100001871 | |
project.funder.identifier | http://doi.org/10.13039/501100001871 | |
project.funder.identifier | http://doi.org/10.13039/501100001871 | |
project.funder.identifier | http://doi.org/10.13039/501100001871 | |
project.funder.name | Fundação para a Ciência e a Tecnologia | |
project.funder.name | Fundação para a Ciência e a Tecnologia | |
project.funder.name | Fundação para a Ciência e a Tecnologia | |
project.funder.name | Fundação para a Ciência e a Tecnologia | |
project.funder.name | Fundação para a Ciência e a Tecnologia | |
project.funder.name | Fundação para a Ciência e a Tecnologia | |
rcaap.rights | openAccess | pt_PT |
rcaap.type | article | pt_PT |
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