Development and characterization of novel pectin rafts for the delivery of ibandronate

Abstract

Bisphosphonates cause irritation of the esophagus and stomach after oral administration. This study was planned to overcome the problems associated with bisphosphonates through the formation of rafts in the stomach and enhance the availability of the drug at the absorption site. A novel pectin raft was developed through the utilization of citrus pectin. The percentage of pectin and profile of neutralization of the raft were investigated. Ibandronate, the polymers and the developed formulation were characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC). The release of ibandronate was investigated in 0.1 N hydrochloric acid (HCl), 0.5 N hydrochloric acid, 1.0 N hydrochloric acid and simulated gastric fluid (SGF), and a cell viability study was performed using Caco-2 cells. The RFF5 formulation contained 94.58% pectin, and the duration of neutralization was 45.41 min. The FTIR and XRD showed the chemical stability and uniform distribution of ibandronate in the raft. The TGA and DSC indicated the thermal stability of the formulation. RFF5 showed 99.95% release of ibandronate at 5 min in SGF. RFF5 showed up to 90.47% cell viability when Caco-2 cells were treated with or without the drug (ibandronate). The developed raft can effectively stop the irritation of the stomach and esophagus caused by ibandronate and improve the availability of the drug at the absorption site.