Spray dried mebendazole-loaded Soluplus-based polymeric micelles for improved biopharmaceutical attributes: in vitro and in vivo studies

The aim of this research was to investigate spray-dried mebendazole (MBZ)-loaded Soluplus-based polymeric micelles (MBZ@PMs) for improved solubility and bioabsorption upon oral administration. Following the MBZ@PM preparation, the formed micellar preparation was examined using FTIR, PXRD, DSC, and TEM techniques to determine its physical and chemical properties. Critical micelle concentration determination studies showed that Soluplus (R) can effectively generate stable polymeric micelles. Particle size analysis demonstrated spherical shape and a particle size of 538.7 +/- 2.129 nm. Solubility studies demonstrated approximately eight times higher solubility of MBZ@PMs vis-a-vis MBZ in PBS pH 6.8 (90.16 +/- 2.54 mu g/mL v/s 11.97 +/- 2.99 mu g/mL). Stability studies confirmed that the size distribution and polydispersity index of the prepared polymeric micelles showed negligible variations. In vitro release studies revealed low MBZ release from MBZ@PMs (9.70 +/- 3.2% in 2 h) at pH 1.2 and sustained (33.3 +/- 3.9%) at PBS pH 6.8 in 48 h. In vivo pharmacokinetic studies showed approximately fourfold higher bioavailability (AUC(0-infinity) 153.81 +/- 24.20 v/s 38.20 +/- 5.55) and 1.5-fold extended half-life of MBZ from MBZ@PMs (2.13 +/- 0.53 v/s 1.44 +/- 0.36). Therefore, these unprecedented Soluplus (R)-based polymeric micelles of Mebendazole can be applied as a potential carrier system to improve the therapeutic efficacy of poorly water-soluble compounds.