Influence of novel carrier Soluplus® on aqueous stability, oral bioavailability, and anticancer activity of Morin hydrate

2018-09-19T16:54:32Z (GMT) by Abhijeet D. Kulkarni Veena S. Belgamwar

Present work demonstrated the influence of novel amphiphilic carrier Soluplus® on the solubility and oral bioavailability of Morin hydrate (MOR). Spray-dried solid dispersions (SSD) were developed using the design of experiment (DoE). Saturation solubility study of the optimized formulation SSD F(7) showed many fold increment in the solubility with acceptable aqueous stability. In vitro drug diffusion kinetics suggested Weibull model to be the best fit. In vitro cytotoxicity assay revealed a significant increase in the anticancer potential compared to innate MOR. Furthermore, SSD F(7) showed 2.27-fold enhancement in the relative bioavailability as compared to MOR.

BCS: biopharmaceutical classification system; MOR: Morin hydrate; SD: solid dispersion; SSD: spray dried solid dispersion; PM: physical mixture; CCD: central composite design; PSD: particle size distribution; PDI: polydispersity index; SEM: scanning electron microscopy; XRD: X-ray diffraction; DSC: differential scanning calorimetry; TGA: thermal gravimetric analysis; DTA: differential thermal analysis; DTG: derivative thermogravimetry; Tg: glass transition temperature; API: active pharmaceutical ingredient; P-gp: permeability glycoprotein; SRB: sulforhodamine B; ADR: adriamycin; DoE: design of experiment