The stratum corneum of various donors differs in particular in the composition of the lipoidal phase. Considering the drug amounts penetrating into the stratum corneum a simple methodology to correlate these differences in the stratum corneum composition with the drug amounts detectable within the s
Polymers effect on estradiol partition coefficient between powdered human stratum corneum and water
โ Scribed by Ronald C. Wester; Xiaoying Hui; Philip G. Hewitt; Jurij Hostynek; Scott Krauser; Thomas Chan; Howard I. Maibach
- Publisher
- John Wiley and Sons
- Year
- 2002
- Tongue
- English
- Weight
- 62 KB
- Volume
- 91
- Category
- Article
- ISSN
- 0022-3549
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โฆ Synopsis
Macromolecules have gained interest as drug entities unto themselves and as transport facilitators to alter initial phases of percutaneous absorption. Two macromolecular polymers (MW 2081 and 2565) were designed to hold cosmetics and drugs to the skin surface by altering initial chemical and skin partitioning. The effect of these polymers on the partition coefficient (PC) of estradiol with powdered human stratum corneum (PHSC) and water was determined. There was no statistically significant effect on the PC when the concentration of estradiol was increased 100-fold (0.028-2.8 microg/mL), when the incubation time was increased from 0 to 24 h, or when PHSC was delipidized. The addition of a liphophilic polymer had no effect on the PC; however, the hydrophilic polymer showed a significant polymer concentration-dependent increase (p < 0.01) in log PC for estradiol concentrations. Thus, a macromolecular chemical has the potential to alter the partitioning of chemical into the outer layers of skin, the first step in percutaneous absorption.
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Phosphatidylcholine (PC)-cholesterol (0 -30 mol%) unilamellar vesicles of several sizes (20 -600 nm) were prepared in buffer (pH 7.4) solutions by sonication or extrusion methods. The vesicle size was measured by a dynamic light-scattering method. Absorption spectra of chlorpromazine (CPZ) and trifl