Dexamethasone acetate microemulsions: formulation and effect on skin permeability
10.16438/j.0513-4870.2015-1154
- VernacularTitle:醋酸地塞米松微乳的制备及对皮肤渗透性的影响
- Author:
Fen MEI
1
;
Wei-dong ZENG
2
;
Tao WAN
2
;
Jie-wei HUANG
1
;
Shuang-hui LUO
1
;
Chuan-bin WU
2
;
Yue-hong XU
2
Author Information
1. Guangzhou Baiyunshan Hejigong Pharmaceutical Co., Ltd, Guangzhou 510410, China
2. School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
dexamethasone acetate;
microemulsion;
percutaneous delivery;
permeability;
stratum corneum
- From:
Acta Pharmaceutica Sinica
2016;51(6):979-
- CountryChina
- Language:Chinese
-
Abstract:
The present project was designed to optimize the microemulsion (ME) formulation of oil in water (O/W) for dexamethasone acetate (DA), and examine its impact on DA percutaneous permeation. The saturated solubility of DA in different oils, surfactants and co-surfactants was tested. The ratio of surfactant to co-surfactant was selected by constructing pseudo three phase diagrams to investigate the maximal microemulsion area. In vitro permeation studies of DA from microemulsion and suspension were performed to optimize the formulation further. Differential scanning calorimetry (DSC) and attenuated total reflection flourier transformed infrared spectroscopy (ATR-FTIR) were performed to investigate the mechanism of microemulsion action on skin. The optimized formulation was composed of oleic acid/Labrasol/propylene glycol/water with 8/45/15/32(w/w), and the DA loading was 0.75% (w/w). The permeation enhancement of microemusion was 6.00-fold as that of suspension, and the DA from microemulsion retained in the skin was 4.79-fold as that of suspension. DSC and ATR-FTIR results suggested that microemulsion could affect the intercellular lipid lamellae and keratin of the stratum corneum. The barrier function of stratum corneum was disordered by the microemulsion so that the dermal drug delivery was enhanced. Therefore, the optimized microemulsion enhanced DA percutaneous permeation significantly through the interaction of microemulsion with skin, microemulsion is a promising approach for DA percutaneous delivery.
