Solubility enhancement of poorly aqueous soluble novel drug using natural gum as carriers

Abstract

The current article is based on the concept to enhance the solubility and dissolution rate of a model drug, Rosuvastatin Calcium, which is BCS class-II drug with anti-hyperlipidemic potential. The reported bioavailability from oral route of drug is only 20%. So aim of current study is to improve the solubility and dissolution rate of a poorly water-soluble drug Rosuvastatin Calcium, by solid dispersion technique. Physical mixtures and solid dispersions were prepared using natural polymers A. Marmelos in different to drug to carrier ratios. Prepared formulations were characterized in solid state by FTIR analysis, powder X-ray diffraction, Scanning electron microscopy and in-vitro dissolution study. Solid state characterizations indicated the Rosuvastatin Calcium was present in amorphous form and entrapped in polymer matrix. In contrast to the very slow dissolution rate of pure Rosuvastatin Calcium, the dispersion of the drug in the polymers considerably enhanced the dissolution rate. The mixtures of solid dispersion and excipients were evaluated for pre-compression parameters. After then fast dissolving tablets were prepared by direct compression technique. The formulated tablets were evaluated by post compression parameters. In-vitro drug release performance of the developed formulations was investigated.

Application of the artificial neural network to optimize the formulation of self-nanoemulsifying drug delivery system containing rosuvastatin

“…In primary approaches, rosuvastatin's solubility, dissolution rate, and bioavailability can be enhanced by decreasing the particle size or nanonization, for example, nanoparticle (Alshora et al, 2018) and nanocrystallization (Palani et al, 2015). In different approaches, rosuvastatin can be formulated into different carriers, such as β-cyclodextrin complexation (Kapse et al, 2016;Sarfraz et al, 2017), cyclodextrin-based nanosponges (Gabr et al, 2018), natural polymers (Kumar Katual et al, 2020), and solid dispersion systems (Mounica et al, 2015). Recently, nanostructured lipid carriers (solid lipid, SNEDDS, and SMEDDS) have been used and they show promising results in improving the solubility of rosuvastatin (Kamble et al, 2014;Li et al, 2018;Rizwanullah et al, 2017).…”