Formulation & Development of nanocomposites for solubility enhancement of BCS Class II model drug using microwave induced diffusion technique

Objective: The oral bioavailability of a specific drug is depends on its solubility and permeability within the Gastro intestinal (GI) tract, which is an aqueous environment. The solubility and bioavailability of BCS Class II drugs can be improved by developing a method reducing the particle size and converting the drug into amorphous state. materials. In the present study nanocomposites (NCs) were formulated using microwave induced diffusion technique (MIND) for solubility enhancement of poorly water soluble (BCS class II) model drug Atorvastatin calcium.

Methods: The nanocomposites of atorvastatin calcium were developed using natural and synthetic carriers such acacia, chitosan, HPMC K4M and avicel 101. Different Physical mixture & nanocomposites formulations were prepared with varying ratios of drug and carriers. The selections of natural & synthetic carriers were based on their surfactant and wetting properties.

Results: In case of developed nanocomposites, the optimum drug-to-carrier ratio was found to be 1:4 with Gum acacia as a carrier which enhanced solubility nearly 15 fold as compared to pure drug. From the dissolution study of the nanocomposites there was evidently a remarkable improvement of the dissolution rate in NCs compared with the pure Atorvastatin calcium was observed. The optimized nanocomposites were characterized by Fourier transform infrared spectroscopy, Differential scanning calorimetry, X-ray diffraction and Scanning electron microscopy.

Conclusion: From Solubility, In vitro drug release and Physical characterization of carriers it is clear that the nanocomposite ATGN4 formulation was found to be optimum in terms of solubility enhancement. The MIND technique employed in this study is green, cost-effective and a promising approach for solubility enhancement.