In Vitro Release Studies on Matrix Type Transdermal Drug Delivery Systems of Naltrexone and Its Acetyl Prodrug

Abstract

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 (M_t) 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 M_t vs. 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.

Key Words:

• Naltrexone
• Prodrugs
• In vitro release testing
• Drug in adhesive patches