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

Abstract

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.

Abbreviations

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; T_g: glass transition temperature; API: active pharmaceutical ingredient; P-gp: permeability glycoprotein; SRB: sulforhodamine B; ADR: adriamycin; DoE: design of experiment

Keywords:

• Morin hydrate
• polyphenols
• solubility enhancement
• Soluplus^®
• spray drying

Acknowledgements

Authors are very grateful to the BASF Corporation Ltd., India for providing a generous gift of Soluplus^® to carry out the research. This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors.

Disclosure statement

All authors have given the consent to the final version of the manuscript. The authors declare no competing financial interest.