Preparation of Fraxetin Long Circulating Liposome and Its Anti-enteritis Effect.
AAPS PharmSciTech
; 22(3): 110, 2021 Mar 17.
Article
em En
| MEDLINE
| ID: mdl-33733385
ABSTRACT
This study sought to improve the oral bioavailability and enhance the anti-enteritis effect of fraxetin by incorporating it into long circulating liposomes (F-LC-Lipo). The optimal formulation of F-LC-Lipo was obtained via orthogonal design. The particle size, morphology, encapsulation efficiency, stability, and anti-enteritis effect of F-LC-Lipo were evaluated. The particle size of F-LC-Lipo was 166.65 ± 8.75 nm with entrapment efficiency (EE) of 92.18 ± 0.17%. The release rate in different dissolution media (pH 1.2 HCl, DDW, and pH 7.4 PBS) was significantly higher than that of fraxetin solution. Compared with the free fraxetin solution, F-LC-Lipo increased oral bioavailability of fraxetin by 4.43 times (443%). More importantly, F-LC-Lipo could improve the levels of interleukin-1 beta (IL-1ß), IL-6, malondialdehyde (MDA), superoxide dismutase (SOD), tumor necrosis factor-alpha (TNF-α), C-reactive protein (CRP), prostaglandin E2 (PEG2), and IL-10 in rats with enteritis. Overall, these results suggested that LC-Lipo may serve as a potential carrier for improving the solubility and oral bioavailability of fraxetin as well as improving its enteritis effect.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Cumarínicos
/
Enterite
/
Antioxidantes
Limite:
Animals
Idioma:
En
Revista:
AAPS PharmSciTech
Assunto da revista:
FARMACOLOGIA
Ano de publicação:
2021
Tipo de documento:
Article
País de afiliação:
China