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Enhanced solubility and biopharmaceutical performance of atorvastatin and metformin via electrospun polyvinylpyrrolidone-hyaluronic acid composite nanoparticles.
European Journal of Pharmaceutical Sciences 2021 March 21
The study was aimed to improve the aqueous solubility of atorvastatin (AT) and ameliorate permeability of metformin (MT) in a combination formulation, improving their oral bioavailability. Several AT-MT loaded polyvinylpyrrolidone (PVP) and hyaluronic acid (HA) based nanoparticles were prepared through electrospraying method (ES-NPs), and tested for physicochemical, in vitro, and in vivo parameters. Among the trialed formulations, a sample consisting of AT, MT, PVP, and HA at the weight ratio of 1/6.25/3.75/15 furnished the most satisfying solubility and release rate results. It enhanced approximately 10.3-fold and 3.6-fold solubility of AT as compared with AT powder and marketed product (Lipilow) in phosphate buffer pH = 6.8, respectively. Whereas, permeation of MT was 1.60-fold and 1.47-fold improved as compared with MT powder and marketed product (Glucophage), respectively. As compared with Lipilow, AUC (0-∞) and Cmax of AT with ES-NPs in rats were improved to 3.6-fold and 3.2-fold, respectively. Similarly, as compared with Glucophage, AUC (0-∞) and Cmax of MT were improved to 2.3-fold and 1.8-fold, respectively. Thus, ES-NPs significantly enhanced the solubility of AT (a BCS class II drug) and permeability of MT (a BCS class III drug) and might be a promising drug delivery system for co-delivery of these drugs.
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