Skin concentrations of thromboxane synthetase inhibitor after topical application with bioelastic membrane.
Elevated thromboxane levels are associated with a number of disease states, including dermal pressure ulcers. When dazmegrel was orally administered to greyhound dogs wearing leg casts, it resulted in a sparring effect on the skin areas of potential pressure ulcer development. The objective of this research was to determine if bioelastic matrices could provide controlled release of thromboxane A2 synthetase inhibitor (dazmegrel) at tissue concentrations sufficient for inhibition of thromboxane synthesis. The animal used for these studies was the greyhound, which has thin skin, angular conformation, limited body fat and is predisposed to pressure ulcers similar to those occurring in humans. In vivo skin penetration studies showed that epidermal exposure to bioelastic thromboxane synthetase inhibitor (TSI) matrix resulted in local tissue concentrations of TSI sufficient for thromboxane synthetase inhibition. There were no significant differences between dazmegrel in the skin layers (epidermis, dermis and subcutaneous layers) on 1, 7 and 14-day exposures.
Wang
N-Z
NZ
Department of Anatomy, Physiology and Pharmacology, College of Veterinary Medicine, Auburn University, Auburn, AL 36849, USA.
Urry
D W
DW
Swaim
S F
SF
Gillette
R L
RL
Hoffman
C E
CE
Hinkle
S H
SH
Coolman
S L
SL
Luan
C-X
CX
Xu
J
J
Kemppainen
B W
BW
D000279:Administration, Cutaneous; D000818:Animals; D004285:Dogs / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005260:Female; D007093:Imidazoles / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D008567:Membranes, Artificial; D003668:Pressure Ulcer / Q000517:prevention & control*; D012867:Skin / Q000378:metabolism*; D013930:Thromboxane-A Synthase / Q000037:antagonists & inhibitors*; D014945:Wound Healing
D004791:Enzyme Inhibitors; D007093:Imidazoles; D008567:Membranes, Artificial; C039242:dazmegrel; D013930:Thromboxane-A Synthase