Development and Characterization of Oral Formulations of Edaravone and Posaconazole for Enhanced Bioavailability

Abstract

The development of safe and efficacious pharmaceutical moieties comes with hefty concerns of low solubility and permeability leading to low bioavailability, which still stands as a challenge to the formulation development of such APIs. Various techniques have helped to improve the bioavailability of such active substance like particle size reduction (micronization and nanonisation) to increase surface area, solid dispersion, polymeric encapsulation, inclusion newlinecomplexation, etc. Present work oral route has been explored for the delivery of the two active pharmaceutical molecules, molecules considered to enhance the bioavailability are newlinePosaconazole and Edaravone using bioavailability enhancement techniques like solid dispersion and encapsulation respectively. Posaconazole solution was formulated via a microemulsion approach, where the API would be encapsulated in micellar globules to improve the solubility and permeability of the molecule. The microemulsion was characterized for zeta newlinepotential, globule size, % drug release, and palatability. The globule size was found to be 74.28 ± 4.1 nm, zeta potential was +12.45 mV, % drug release was more than 90% in 30 minutes and palatability was good and the formulation was stable for six months. An In-vitro release study of the Posaconazole formulation and marketed formulation was carried out. Solid dispersion of Edaravone in drug-polymer dispersion was prepared and solubilized in a carrier solution which is absorbed on the carrier to yield granules filled in a HGC to improve bioavailabity of newlinethe Edaravone. The formulation was characterized for % drug release, assay and related substance. The % drug release was achieved more than 98%, the assay was more than 95% and the impurity level was less than 1.0%. The formulation was stable for six months. The in-vivo study depicted the novel formulation was comparable to the marketed formulation in terms of efficacy.