A pre‑formulation study of tetracaine loaded in optimized nanostructured lipid carriers
Carregando...
Data
Data de publicação
Autores IPEN
Orientador
Título da Revista
ISSN da Revista
Título do Volume
É parte de
É parte de
É parte de
Scientific Reports
Exportar
Resumo
Tetracaine (TTC) is a local anesthetic broadly used for topical and spinal blockade, despite its systemic toxicity. Encapsulation in nanostructured lipid carriers (NLC) may prolong TTC delivery at the site of injection, reducing such toxicity. This work reports the development of NLC loading 4% TTC. Structural properties and encapsulation efficiency (%EE > 63%) guided the selection of three pre-formulations of different lipid composition, through a 23 factorial design of experiments (DOE). DLS and TEM analyses revealed average sizes (193–220 nm), polydispersity (< 0.2), zeta potential |− 21.8 to − 30.1 mV| and spherical shape of the nanoparticles, while FTIR-ATR, NTA, DSC, XRD and SANS provided details on their structure and physicochemical stability over time. Interestingly, one optimized pre-formulation (CP-TRANS/TTC) showed phase-separation after 4 months, as predicted by Raman imaging that detected lack of miscibility between its solid (cetyl palmitate) and liquid (Transcutol) lipids. SANS analyses identified lamellar arrangements inside such nanoparticles, the thickness of the lamellae been decreased by TTC. As a result of this combined approach (DOE and biophysical techniques) two optimized pre-formulations were rationally selected, both with great potential as drug delivery systems, extending the release of the anesthetic (> 48 h) and reducing TTC cytotoxicity against Balb/c 3T3 cells.
Como referenciar
CASTRO, SIMONE R.; RIBEIRO, LIGIA N.M.; BREITKREITZ, MARCIA C.; GUILHERME, VIVIANE A.; SILVA, GUSTAVO H.R. da; MITSUTAKE, HERY; ALCANTARA, ANA C.S.; YOKAICHIYA, FABIANO; FRANCO, MARGARETH K.K.D.; CLEMENS, DANIEL; KENT, BEN; LANCELLOTTI, MARCELO; ARAUJO, DANIELE R. de; PAULA, ENEIDA de. A pre‑formulation study of tetracaine loaded in optimized nanostructured lipid carriers. Scientific Reports, v. 11, n. 1, p. 1-15, 2021. DOI: 10.1038/s41598-021-99743-6. Disponível em: http://repositorio.ipen.br/handle/123456789/32392. Acesso em: 20 Mar 2026.
Esta referência é gerada automaticamente de acordo com as normas do estilo IPEN/SP (ABNT NBR 6023) e recomenda-se uma verificação final e ajustes caso necessário.