Microemulsions formed by PPG-5-CETETH-20 at low concentrations for transdermal delivery of nifedipine: Structural and in vitro study.

Autor: Souza de Araujo GR; Department of Pharmacy, Federal University of Sergipe, Av. Marechal Rondon, Jd. Rosa Elze, São Cristóvão, s/n 49100-000 SE, Brazil., Mendonça da Cruz Macieira G; Department of Chemistry, Federal University of Sergipe, Av. Vereador Olimpio Grande, Sítio Porto, Itabaiana, s/n 49506-036 SE, Brazil., Xavier de Oliveira D; Department of Chemistry, Federal University of Sergipe, Av. Vereador Olimpio Grande, Sítio Porto, Itabaiana, s/n 49506-036 SE, Brazil., Santos Matos S; Department of Pharmacy, Federal University of Sergipe, Av. Marechal Rondon, Jd. Rosa Elze, São Cristóvão, s/n 49100-000 SE, Brazil., Nery Dos Santos Q; Department of Pharmacy, Federal University of Sergipe, Av. Marechal Rondon, Jd. Rosa Elze, São Cristóvão, s/n 49100-000 SE, Brazil., Otubo L; Instituto de Pesquisas Energéticas e Nucleares, IPEN/CNEN, Cidade Universitária, Av. Prof. Lineu Prestes, 2242, São Paulo, CEP 05508-000 SP, Brazil., Antunes de Souza Araújo A; Department of Pharmacy, Federal University of Sergipe, Av. Marechal Rondon, Jd. Rosa Elze, São Cristóvão, s/n 49100-000 SE, Brazil., Cavalcante Duarte M; Department of Pharmacy, Federal University of Sergipe, Av. Marechal Rondon, Jd. Rosa Elze, São Cristóvão, s/n 49100-000 SE, Brazil., Moreira Lira AA; Department of Pharmacy, Federal University of Sergipe, Av. Marechal Rondon, Jd. Rosa Elze, São Cristóvão, s/n 49100-000 SE, Brazil., de Souza Nunes R; Department of Pharmacy, Federal University of Sergipe, Av. Marechal Rondon, Jd. Rosa Elze, São Cristóvão, s/n 49100-000 SE, Brazil., Vitorino Sarmento VH; Department of Chemistry, Federal University of Sergipe, Av. Vereador Olimpio Grande, Sítio Porto, Itabaiana, s/n 49506-036 SE, Brazil. Electronic address: vhsarmento@academico.ufs.br.
Jazyk: angličtina
Zdroj: Colloids and surfaces. B, Biointerfaces [Colloids Surf B Biointerfaces] 2022 Jun; Vol. 214, pp. 112474. Date of Electronic Publication: 2022 Mar 23.
DOI: 10.1016/j.colsurfb.2022.112474
Abstrakt: Nifedipine is a potent anti-hypertensive, which is poorly orally bioavailable on account of first-pass metabolism, short half-life, and low water solubility. This study aimed to develop a microemulsified system with low surfactant concentration and to evaluate the influence of microemulsion (ME) phase behavior on skin permeation of nifedipine, as drug model. Thereafter, MEs were obtained using PPG-5-CETETH-20, oleic acid, and phosphate buffer at pH 5.0. The selected MEs were isotropic, with droplet diameters less than 10 nm, polydispersity index < 0.25, and pH between 5.0 and 5.2. MEs presented low viscosity and Newtonian behavior. SAXS results confirmed bicontinuous and oil-in-water (o/w) MEs formation. The presence of the drug promoted only very slight modifications in the ME structure. The MEs presented ability to deliver nifedipine via the transdermal route when in comparison with the control. Nevertheless, the skin permeated and retained amounts from the o/w and bicontinuous formulations did not differ significantly. The ATR-FTIR demonstrated that both formulations promoted fluidization and disorganization of lipids and increased the drug diffusion and partition coefficients in the skin. In conclusion, PPG-5-CETETH-20 MEs obtained proved to be effective skin permeation enhancers, acting by rising the coefficients of partition and diffusion of the nifedipine in the skin.
(Copyright © 2022 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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