| Texto completo | |
| Autor(es): Mostrar menos - |
Souza, A. D.
;
da Silva, G. H. Rodrigues
;
Ribeiro, L. N. M.
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Mitsutake, H.
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Bordallo, H. N.
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Breitkreitz, M. C.
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Fernandes, P. C. Lima
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Moura, L. D.
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Yokaichiya, F.
;
Franco, M.
;
de Paula, E.
Número total de Autores: 11
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| Tipo de documento: | Artigo Científico |
| Fonte: | ACS BIOMATERIALS SCIENCE & ENGINEERING; v. 10, n. 8, p. 12-pg., 2024-07-29. |
| Resumo | |
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 2(3) 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 degrees 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. (AU) | |
| Processo FAPESP: | 19/17784-0 - Análise farmacocinética e de distribuição local no tecido-alvo de fármacos encapsulados em sistemas carreadores baseados em lipídios |
| Beneficiário: | Eneida de Paula |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |