Design of an Ante-enhancer with an Azone-Mimic Structure using Ionic Liquid.
Pharm Res
; 40(6): 1577-1586, 2023 Jun.
Article
en En
| MEDLINE
| ID: mdl-37081304
ABSTRACT
PURPOSE:
Laurocapram (Azone) was broadly examined as a representative enhancer of skin penetration in the 1980s. However, it was not approved for treatment because it caused skin irritation following its penetration into the epidermis through the stratum corneum. In the present study, a so-called ante-enhancer with an Azone-mimic structure was designed based on an ante-drug with negligible systemic toxic effects following its permeation through the skin.METHODS:
The ante-enhancer was designed using ionic liquid technology an ionic liquid-type ante-enhancer (IL-Azone) with an Azone-mimic structure was prepared from ε-caprolactam and myristic acid as cationic and anionic substances, respectively. The enhancing effects of IL-Azone on the permeation by the following model drugs through pig skin were examined isosorbide 5-mononitrate (ISMN), antipyrine (ANP), and fluorescein isothiocyanate dextran (FD-4). Skin irritation by IL-Azone was assessed using the Draize method.RESULTS:
The primary irritation index (P.I.I.) of IL-Azone by the Draize method was markedly lower than that of Azone (6.9). Although the ability of IL-Azone to enhance skin penetration was not as high as Azone, IL-Azone moderately increased skin permeation by the model compounds tested (ISMN 4.7 fold, ANP 4.5 fold, FD-4 4.0 fold).CONCLUSIONS:
These results suggest the usefulness of designing a skin penetration enhancer using ionic liquid technology. Further trials on the ionic liquid design with an Azone-mimic structure using other cations and anions may lead to the development of better ante-enhancers.Palabras clave
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Absorción Cutánea
/
Líquidos Iónicos
Límite:
Animals
Idioma:
En
Revista:
Pharm Res
Año:
2023
Tipo del documento:
Article
País de afiliación:
Japón