In vitro release studies on matrix type transdermal drug delivery systems of naltrexone and its acetyl prodrug.
Matrix type acrylic adhesive transdermal patches of naltrexone (NTX) and its 3-O-acetyl ester prodrug were prepared and evaluated for drug content, thickness, and in vitro release characteristics. Among the four DURO-TAK adhesive polymers (87-2516, 87-2054, 87-2501, and 87-2582) tested, 87-2516 proved to be the most suitable and compatible polymer for the transdermal delivery of NTX from NTX and prodrug patches. A linear relationship was observed for release flux (F) and cumulative amount (Mt) values versus 1%, 2%, and 3% drug loading at equimolar levels. The release of NTX from the patches showed a good correlation (R2>0.99) for Mt vs. square root t profiles, indicating that a Higuchian matrix diffusion mechanism of drug release from the transdermal adhesive patches was obtained. Overall, the amounts of NTX released from the prodrug patches were significantly higher than from the NTX patches, at all three drug loading levels.
Nalluri
Buchi N
BN
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky 40536-0082, USA.
Milligan
Caitlin
C
Chen
Jianhong
J
Crooks
Peter A
PA
Stinchcomb
Audra L
AL
D000107:Acetylation; D000279:Administration, Cutaneous; D000465:Algorithms; D002851:Chromatography, High Pressure Liquid; D004058:Diffusion; D009271:Naltrexone / Q000008:administration & dosage* / Q000737:chemistry; D009292:Narcotic Antagonists / Q000008:administration & dosage* / Q000737:chemistry; D011355:Prodrugs / Q000008:administration & dosage* / Q000737:chemistry; D012997:Solvents; D013056:Spectrophotometry, Ultraviolet
D009292:Narcotic Antagonists; D011355:Prodrugs; D012997:Solvents; D009271:Naltrexone