Design and Evaluation of Atazanavir Bi Sulfate Nanosuspension

摘要

Nano sizing refers to the reducing the size of active Pharmaceutical Ingredient (API) to micron range up to below 1 μm typically a few hundred nanometers.1 The sub-micron particles are stabilized with surfactants or polymers in NSs, which can be further processed into standard dosage forms, such as capsules or tablets, suitable for oral administration. These nano formulations offer increased dissolution rates and enhance bioavailability of insoluble compounds (BCS Class II and IV drugs). NSs efficiently improve oral absorption of poorly soluble drugs and achieve a higher bioavailability compared to traditional formulation. Present study has been undertaken to develop NS of ATV, by media milling method, with improved oral bioavailability. Formulation of NS requires a careful selection of stabilizers. Steric and electrostatic stabilizers are needed to stabilize the nanoparticles against inter-particle forces and prevent them from aggregating. Steric stabilization is often combined with electrostatic stabilization for additional repulsive contribution. Different pharmaceutical excipients including povidone (PVP K25), poloxamer and steric stabilizer and sodium lauryl sulphate (SLS) as anionic electroststic stabilizer were used in an effort to develop stable ATV loaded NS.