Transdermal absorption of radioprotectors using permeation-enhancing vehicles
- Temple Univ. School of Medicine, Philadelphia, PA (USA)
Radioprotectors are not currently used clinically due to concerns regarding toxicity and uncertainties regarding tumor protection. Topical radioprotection of skin might find clinical applications with protectors such as WR-2721, but laboratory studies in which protectors have been applied in water have not been promising. We have studied the absorption of 14C-WR-2721 and ({sup 14}C)cysteine dissolved in skin permeation-enhancing vehicles through the skin of hairless mice and compared the absorption to that in water. Skin concentration of WR-2721 was increased most by dimethylformamide (DMF), but only propylene glycol increased absorption as far as the dermis, as measured by plasma concentration. Skin concentration of cysteine was improved by DMF, 2-pyrrolidone (2-P), and methyl-2-pyrrolidone (M-2-P); only dimethylsulfoxide (DMSO) resulted in increased plasma levels of the protector. Pretreating skin with DMSO before application of WR-2721, irrespective of the vehicle, improved its concentration within the skin. Plasma levels were improved (10 and 12 times) only with 2-P and DMF. Therefore, by choosing the appropriate vehicle, it is possible to breach the barrier of the stratum corneum and enhance the presence of the protector in all layers of the skin.
- OSTI ID:
- 6936735
- Journal Information:
- Radiation Research; (USA), Vol. 121:2; ISSN 0033-7587
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
59 BASIC BIOLOGICAL SCIENCES
RADIOPROTECTIVE SUBSTANCES
SKIN ABSORPTION
CARBON 14 COMPOUNDS
CYSTEINE
MICE
NEOPLASMS
TRACER TECHNIQUES
ABSORPTION
AMINO ACIDS
ANIMALS
CARBOXYLIC ACIDS
DISEASES
DRUGS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANIC SULFUR COMPOUNDS
RODENTS
THIOLS
UPTAKE
VERTEBRATES
560152* - Radiation Effects on Animals- Animals
550901 - Pathology- Tracer Techniques