Drug Eluting Device References

Intravaginal rings (IVRs) have emerged as cost effective way to deliver sustained release of drugs as compared to vaginal gels. Hydrophobic polyether polyurethane Intravaginal rings (IVRs) were investigated to deliver antiretroviral (ARV) drug in combination with a HIV reverse transcriptase inhibitor. The ARV used was N-[2-(3,4,5-trumethoxybenzoilthio)benzoyl]-alaninamide (SAMT-10) and the HIV-1 reverse-transcriptase inhibitor used was pyrimidinedinone IQP-0528. SAMT’s are generally known to be hydrolytically unstable due to the thioester bond which poses a challenge to the design of the delivery system being used. Incorporation of the SAMT-10 and the IQP-0528 into the IVR by extrusion resulted in a matrix design. The drug loaded IVR’s when subjected to accelerated stability conditions of 40oC/75%RH showed no degradation of the hydrolytically labile SAMT-10. The polyurethane matrix protects and prevents the degradation of SAMT-10. Further toxicological evaluations of these IVR’s indicated no evidence of formulation toxicity. SAMT-10 and IQP-0528 had different solubility in the polyurethane matrix, SAMT-10 had lower solubility. Presence of IQP-0528 increased the overall diffusivity of SAMT-10, whereas, the release of IQP-0528 was inhibited by the limited solubility of SAMT-10 in the matrix. Physical properties such as compression force of the IVR with the combination drugs was similar to the well accepted NuvaRing®. The study concluded that a sustained release of ARV in combination with a dual-acting entry inhibitor, IQP-0528, can be obtained through a polyurethane IVR.