CaCO3 MICROPARTICLE CONTAINING IBANDRONATE–ALGINATE BEADS FOR IMPROVED ADHERENCE TO BISPHOSPHONATE ORAL THERAPY: FORMULATION AND IN-VITRO RELEASE

Bisphosphonates are established as supportive therapy to reduce the frequency and severity of cancer-related skeletal complications. Oral formulations are preferred over intravenous if the patients are not hospitalized. The maximum absorption of oral bisphosphonates takes place in stomach. The adverse events with oral dosing are seen in buccal mucosa and gastrointestinal tract, which lead to poor adherence to bisphosphonates therapy. In the present study different ibandronate-alginate beads were formulated and characterized for physiochemical parameters like shape, effect of ibandronate and alginate content, encapsulation of drug and drug release. CaCO3 microparticles were incorporated in ibandronate-alginate formulations and studied for increased ibandronate release in simulated gastric fluid (SGF). The ibandronate encapsulation in all formulations was high and was independent on the amount of drug encapsulated. The release of ibandronate from ibandronate-alginate beads was dependent on alginate concentration and not on the amount of drug encapsulated. Additionally, the drug release was more in simulated intestinal fluid (SIF) than in SGF. However, the incorporation of CaCO3 microparticles in ibandronate–alginate beads increased the release of drug in SGF. The scanning electron microscope studies of CaCO3 microparticles containing ibandronate– alginate beads, after incubation in SGF, demonstrated the presence of tiny pores on the surface as well as within the beads. These beads also exhibited increased and sustained ibandronate release in SGF.