Sammeta, S. M., Wang, L., Mutyam, S. K., O’Loughlin, K., Green, C. E., Werner, M. H., . . . Shankar, G. N. (2015). Formulation approaches to improving the delivery of an antiviral drug with activity against seasonal flu. Pharmaceutical Development and Technology, 20(2), 169-175. doi: 10.3109/10837450.2013.852574
The main objective of the present study was to develop formulations of noscapine hydrochloride hydrate with enhanced solubility and bioavailability using co-solvent- and cyclodextrin-based approaches. Different combinations of co-solvents, which were selected on the basis of high-throughput solubility screening, were subjected to in vitro intestinal drug permeability studies conducted with Ussing chambers. Vitamin E tocopherol polyethylene glycol succinate and propylene glycol based co-solvent formulations provided the maximum permeability coefficient for the drug. Inclusion complexes of the drug were prepared using hydroxypropyl-β-cyclodextrin and sulphobutylether cyclodextrins. Pharmacokinetic studies were carried out in male Sprague-Dawley rats for the selected formulations. The relative bioavailabilities of the drug with the co-solvent- and cyclodextrin-based formulations were found to be similar.