Therapeutic Polymers to Deter Intravenous Drug Abuse

Nova Southeastern University, Davie, Florida, USA

Objective. This study was conducted to determine the percentage of Dextromethorphan HBr (DEX) that could be extracted in solutions from drug-loaded therapeutic polymers (AcDiSol and Explotab) and compare to physical blends of the same. Background. Currently marketed intravenous abuse-deterrent formulations are either crush-resistant or extraction-resistant (by forming viscous gels in solutions), each of which abusers could manipulate. In this work, we developed a new extraction-resistant approach, using drug-loaded therapeutic polymers. The drug loads are expected to remain complexed to the polymers when drug formulations are manipulated in various solvents. Methods. DEX-AcDiSol/Explotab (1:8) complexes were prepared in water. The complexes were dried and milled, and amounts equivalent to 25 mg DEX were dispersed in 10 mL aqueous solutions. The % drug in solution was determined via UV spectrophotometer. The deterrence efficiency was compared to physical mixtures of the same. Results. Drug extraction from both therapeutic polymers was < 10% in polar solvents and 40% v/v ethanol. Solvents with ions could extract > 50% of the drug, the AcDiSol therapeutic polymer being more susceptible with ~ 80% drug extraction in normal saline. Compared to their physical blends, AcDiSol and Explotab therapeutic polymers were ~ 10% and ~ 25% more effective in reducing drug extraction in polar solvents, respectively, and ~ 35% more effective in ethanol. Conclusion. While therapeutic polymers of DEX-loaded AcDiSol and Explotab significantly reduced drug extraction in polar and alcoholic solutions, further work is needed to overcome their vulnerability to ions. Grants. This study was funded by NSU grant 335081.