Use of Nanohybrid Material for Formulation, Development and Evaluation of Pharmaceutical Dosage Form Containing the Low Solubility Active Pharmaceutical Ingredient

Abstract

In oral absorption of a drug, the drug first dissolves and then is absorbed by diffusion through gastrointestinal membranes. The gastrointestinal environment is aqueous in nature and it is well-known that one-third of the drug population is water insoluble. Hence, there is a need for enhancement of the solubility and dissolution of such drugs. In this work, enhancement of the solubility and dissolution of the practically insoluble drug Rosuvastatin Calcium was achieved by formation of nanohybrids using microwave-induced diffusion (MIND), which ultimately leads to bioavailability enhancement. nanohybrids were formed by using natural carriers such as acacia,guar gum and PVP k-30 with the help of microwaves. Selection of carriers was based on their surfactant and wetting properties. Solubility studies were carried out to establish the solubility-enhancing property of the nanohybrids. To support solubility analysis results, dissolution studies (i.e. powder dissolution and in-vitro dissolution) were carried out. The nanohybrids were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction studies, scanning electron microscopy and transmission electron microscopy. It was found that as the concentration of polymer in the composite increased the solubility and dissolution of rosuvastatin calcium were enhanced. The optimised ratio (drug : polymer) for all the composites was found to be 1:4. The novelty of this work is the green and cost-effective way of forming drug nanocomposites with the help of microwave, which can be scaled up to an industrial level. The method gives an immaculate means of solubilisation by generating drug dispersion at the micro and nanoscale level in natural biodegradable stabilising media. Hence, this study demonstrates the use of nanohybrids in solubility and dissolution enhancement.
 Keywords- BCS Class II, Nanohybrids, Solubilization, Enhancement of solubility, Optimized drug dissolution and drug release.