Fresh carrier for an old topical local anesthetic
dc.contributor.author | SOUZA, A.D. | |
dc.contributor.author | SILVA, G.H.R. da | |
dc.contributor.author | RIBEIRO, L.N.M. | |
dc.contributor.author | MITSUTAKE, H. | |
dc.contributor.author | BORDALLO, H.N. | |
dc.contributor.author | BREITKREITZ, M.C. | |
dc.contributor.author | FERNANDES, P.C.L. | |
dc.contributor.author | MOURA, L.D. | |
dc.contributor.author | YOKAICHIYA, F. | |
dc.contributor.author | FRANCO, M. | |
dc.contributor.author | PAULA, E. de | |
dc.coverage | Internacional | |
dc.date.accessioned | 2024-12-12T15:00:34Z | |
dc.date.available | 2024-12-12T15:00:34Z | |
dc.date.issued | 2024 | |
dc.description.abstract | Nanostructured 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.sponsorship | Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) | |
dc.description.sponsorship | Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) | |
dc.description.sponsorship | Carlsberg Foundation (CF) | |
dc.description.sponsorshipID | FAPESP: 19/17784-0 | |
dc.description.sponsorshipID | CNPq: 309625/2017 | |
dc.description.sponsorshipID | CF: 19-0521 | |
dc.format.extent | 4958-4969 | |
dc.identifier.citation | SOUZA, 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.doi | 10.1021/acsbiomaterials.4c00585 | |
dc.identifier.fasciculo | 8 | |
dc.identifier.issn | 2373-9878 | |
dc.identifier.percentilfi | 74.5 | |
dc.identifier.percentilfiCiteScore | 82.50 | |
dc.identifier.uri | https://repositorio.ipen.br/handle/123456789/48756 | |
dc.identifier.vol | 10 | |
dc.relation.ispartof | ACS Biomaterials Science and Engineering | |
dc.rights | openAccess | |
dc.subject | anesthesia | |
dc.subject | anesthetics | |
dc.subject | paba | |
dc.subject | drug delivery | |
dc.subject | nanoparticles | |
dc.title | Fresh carrier for an old topical local anesthetic | |
dc.type | Artigo de periódico | |
dspace.entity.type | Publication | |
ipen.autor | MARGARETH KAZUYO KOBAYASHI DIAS FRANCO | |
ipen.codigoautor | 9803 | |
ipen.contributor.ipenauthor | MARGARETH KAZUYO KOBAYASHI DIAS FRANCO | |
ipen.identifier.fi | 5.5 | |
ipen.identifier.fiCiteScore | 10.3 | |
ipen.identifier.ipendoc | 30782 | |
ipen.identifier.iwos | WoS | |
ipen.range.fi | 4.500 - 5.999 | |
ipen.range.percentilfi | 50.00 - 74.99 | |
ipen.subtitulo | benzocaine in nanostructured lipid carriers | |
ipen.type.genre | Artigo | |
relation.isAuthorOfPublication | ea01b86e-8435-405e-874c-d0b68fb2b549 | |
relation.isAuthorOfPublication.latestForDiscovery | ea01b86e-8435-405e-874c-d0b68fb2b549 | |
sigepi.autor.atividade | MARGARETH KAZUYO KOBAYASHI DIAS FRANCO:9803:1120:N |