Bioavailability Enhancement of Alendronate by Nanoparticle Formulation for Treatment of Osteoporosis

Abstract

Alendronate was selected for this study to improve the bioavailability to treat osteoporosis efficiently by developing nanocarrier system like nanoparticles. This drug belong to the BCS class III in which permeability of drug through gastrointestinal mucosa is the limiting factor to show high bioavailability. Despite their advantages bisphosphonates suffer from very poor bioavailability, serious interferences of absorption by foods and beverages other than water and side effects that consist of irritation to the upper gastrointestinal mucosa. To overcome these limitations bisphosphonates are given in a relatively large dose in a fasting condition while maintaining an upright position for at least half an hour after dosing. The standard treatment with bisphosphonates is chronic and daily so the inconvenience to the patient can lead to non compliance with the dosage regimen. Since bisphosphonates are not metabolized, dosing can be reduced to once a week by administering very large sustained release doses of the drug. But while large dosing helps improve patient compliance, it has the potential of exacerbating the upper GI side effects of the drug. An effort was done to formulate and evaluate the nanocarriers of bisphosphonates for improving the permeability and hence the bioavailability for the better and efficient treatment of osteoporosis. Ionotropic gelation method was used to develop the polymeric nanoparticles. The work demonstrated that drug entrapment and particle size vary with the different concentration of polymer chitosan and Sodium Tri polyphosphate in nanoparticles.