Fresh carrier for an old topical local anesthetic

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dc.contributor.authorSOUZA, A.D.
dc.contributor.authorSILVA, G.H.R. da
dc.contributor.authorRIBEIRO, L.N.M.
dc.contributor.authorMITSUTAKE, H.
dc.contributor.authorBORDALLO, H.N.
dc.contributor.authorBREITKREITZ, M.C.
dc.contributor.authorFERNANDES, P.C.L.
dc.contributor.authorMOURA, L.D.
dc.contributor.authorYOKAICHIYA, F.
dc.contributor.authorFRANCO, M.
dc.contributor.authorPAULA, E. de
dc.coverageInternacional
dc.date.accessioned2024-12-12T15:00:34Z
dc.date.available2024-12-12T15:00:34Z
dc.date.issued2024
dc.description.abstractNanostructured lipid carriers (NLC) have emerged as innovative drug delivery systems, offering distinct advantages over other lipid-based carriers, such as liposomes and solid lipid nanoparticles. Benzocaine (BZC), the oldest topical local anesthetic in use, undergoes metabolism by pseudocholinesterase, leading to the formation of p-aminobenzoic acid, a causative agent for allergic reactions associated with prolonged BZC usage. In order to mitigate adverse effects and enhance bioavailability, BZC was encapsulated within NLC. Utilizing a 23 factorial design, formulations comprising cetyl palmitate (solid lipid), propylene glycol monocaprylate (liquid lipid), and Pluronic F68 as surfactants were systematically prepared, with variations in the solid/liquid lipid mass ratios (60:40-80:20%), total lipid contents (15-25%), and BZC concentrations (1-3%). The optimized formulation underwent characterization by dynamic light scattering, differential scanning calorimetry, Raman imaging, X-ray diffraction, small-angle neutron scattering, nanotracking analysis, and transmission electron microscopy (TEM)/cryo-TEM, providing insights into the nanoparticle structure and the incorporation of BZC into its lipid matrix. NLCBZC exhibited a noteworthy encapsulation efficiency (%EE = 96%) and a 1 year stability when stored at 25 °C. In vitro kinetic studies and in vivo antinociceptive tests conducted in mice revealed that NLCBZC effectively sustained drug release for over 20 h and prolonged the anesthetic effect of BZC for up to 18 h. We therefore propose the use of NLCBZC to diminish the effective anesthetic concentration of benzocaine (from 20 to 3% or less), thus minimizing allergic reactions that follow the topical administration of this anesthetic and, potentially, paving the way for new routes of BZC administration in pain management.
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipCarlsberg Foundation (CF)
dc.description.sponsorshipIDFAPESP: 19/17784-0
dc.description.sponsorshipIDCNPq: 309625/2017
dc.description.sponsorshipIDCF: 19-0521
dc.format.extent4958-4969
dc.identifier.citationSOUZA, A.D.; SILVA, G.H.R. da; RIBEIRO, L.N.M.; MITSUTAKE, H.; BORDALLO, H.N.; BREITKREITZ, M.C.; FERNANDES, P.C.L.; MOURA, L.D.; YOKAICHIYA, F.; FRANCO, M.; PAULA, E. de. Fresh carrier for an old topical local anesthetic: benzocaine in nanostructured lipid carriers. <b>ACS Biomaterials Science and Engineering</b>, v. 10, n. 8, p. 4958-4969, 2024. DOI: <a href="https://dx.doi.org/10.1021/acsbiomaterials.4c00585">10.1021/acsbiomaterials.4c00585</a>. Disponível em: https://repositorio.ipen.br/handle/123456789/48756.
dc.identifier.doi10.1021/acsbiomaterials.4c00585
dc.identifier.fasciculo8
dc.identifier.issn2373-9878
dc.identifier.percentilfi74.5
dc.identifier.percentilfiCiteScore82.50
dc.identifier.urihttps://repositorio.ipen.br/handle/123456789/48756
dc.identifier.vol10
dc.relation.ispartofACS Biomaterials Science and Engineering
dc.rightsopenAccess
dc.subjectanesthesia
dc.subjectanesthetics
dc.subjectpaba
dc.subjectdrug delivery
dc.subjectnanoparticles
dc.titleFresh carrier for an old topical local anesthetic
dc.typeArtigo de periódico
dspace.entity.typePublication
ipen.autorMARGARETH KAZUYO KOBAYASHI DIAS FRANCO
ipen.codigoautor9803
ipen.contributor.ipenauthorMARGARETH KAZUYO KOBAYASHI DIAS FRANCO
ipen.identifier.fi5.5
ipen.identifier.fiCiteScore10.3
ipen.identifier.ipendoc30782
ipen.identifier.iwosWoS
ipen.range.fi4.500 - 5.999
ipen.range.percentilfi50.00 - 74.99
ipen.subtitulobenzocaine in nanostructured lipid carriers
ipen.type.genreArtigo
relation.isAuthorOfPublicationea01b86e-8435-405e-874c-d0b68fb2b549
relation.isAuthorOfPublication.latestForDiscoveryea01b86e-8435-405e-874c-d0b68fb2b549
sigepi.autor.atividadeMARGARETH KAZUYO KOBAYASHI DIAS FRANCO:9803:1120:N
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