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Lipid nanoparticles loaded with butamben and designed to improve anesthesia at inflamed tissues.
Rodrigues da Silva, Gustavo H; Lemes, Julia Borges Paes; Geronimo, Gabriela; Freitas de Lima, Fernando; de Moura, Ludmilla David; Carvalho Dos Santos, Ariany; Carvalho, Nathalia Santos; Malange, Kauê Franco; Breitkreitz, Márcia C; Parada, Carlos A; de Paula, Eneida.
Afiliação
  • Rodrigues da Silva GH; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, São Paulo, Brazil. depaula@unicamp.br.
  • Lemes JBP; Department of Structural and Functional Biology, Institute of Biology, UNICAMP, Brazil.
  • Geronimo G; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, São Paulo, Brazil. depaula@unicamp.br.
  • Freitas de Lima F; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, São Paulo, Brazil. depaula@unicamp.br.
  • de Moura LD; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, São Paulo, Brazil. depaula@unicamp.br.
  • Carvalho Dos Santos A; Faculty of Health Sciences, Federal University of Grande Dourados, Dourados, MS, Brazil.
  • Carvalho NS; Department of Structural and Functional Biology, Institute of Biology, UNICAMP, Brazil.
  • Malange KF; Department of Structural and Functional Biology, Institute of Biology, UNICAMP, Brazil.
  • Breitkreitz MC; Department of Analytical Chemistry, Institute of Chemistry, UNICAMP, Brazil.
  • Parada CA; Department of Structural and Functional Biology, Institute of Biology, UNICAMP, Brazil.
  • de Paula E; Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas - UNICAMP, Campinas, São Paulo, Brazil. depaula@unicamp.br.
Biomater Sci ; 9(9): 3378-3389, 2021 May 04.
Article em En | MEDLINE | ID: mdl-33949447
The most frequently used local anesthetics (LA) for local infiltration have an ionizable amine in the range of pH 7.6-8.9. Effective anesthesia of inflamed tissues is a great challenge, especially because the induced local acidosis decreases the fraction of the neutral (more potent) LA species in situ. To solve this limitation, the butyl-substituted benzocaine analogue butamben (BTB) - that has no ionizable amine group close to the physiological pH - could be useful if it was not for its low solubility. To overcome the solubility problem, an optimized formulation for BTB using nanostructured lipid carriers (NLC) was developed by a factorial design and characterized using DLS, XRD, DSC and cryo-EM. The release kinetics and cytotoxicity of the new formulation were measured in vitro, while the in vivo tests assessed its effectiveness on healthy and inflamed tissues, in rats. The optimized NLCBTB formulation showed desirable physicochemical properties (size = 235.6 ± 3.9 nm, polydispersity = 0.182 ± 0.006 and zeta potential = -23.6 ± 0.5 mV), high (99.5%) encapsulation efficiency and stability during 360 days of storage at room temperature. NLCBTB prolonged the release of butamben and decreased its in vitro cytotoxicity without inducing any in vivo toxic alteration. In the inflammatory hyperalgesia model, the NLCBTB formulation showed potential for the management of inflammatory pain, displaying greater analgesic effectiveness (40%) and a prolonged effect.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Nanoestruturas / Nanopartículas / Anestesia Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Biomater Sci Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Nanoestruturas / Nanopartículas / Anestesia Tipo de estudo: Prognostic_studies Limite: Animals Idioma: En Revista: Biomater Sci Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido