Enhanced buccal mucosal retention and reduced buccal permeability of estradiol in the presence of padimate O and Azone®: A mechanistic study
✍ Scribed by Joseph A. Nicolazzo; Barry L. Reed; Barrie C. Finnin
- Publisher
- John Wiley and Sons
- Year
- 2005
- Tongue
- English
- Weight
- 153 KB
- Volume
- 94
- Category
- Article
- ISSN
- 0022-3549
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✦ Synopsis
In previous experiments, it was suggested that the reduction in estradiol (E 2 ) buccal permeability after pretreatment with some skin penetration enhancers was attributed to enhanced membrane storage. To verify this, further in vitro permeability experiments were performed and the kinetics of E 2 buccal mucosal uptake and permeability was assessed. Porcine buccal mucosa was pretreated with the skin penetration enhancers octisalate, padimate O (PO), or Azone 1 (AZ) and placed in modified Ussing chambers. The disappearance of E 2 from the donor chamber and appearance of E 2 in the receptor chamber was then monitored over 4 h. The final concentration of E 2 associated with the buccal mucosa and donor chamber walls in the presence of each enhancer was also determined. The rate of E 2 disappearance from the donor chamber was 3.