Formulation approaches to improving the delivery of an antiviral drug with activity against seasonal flu

Abstract 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...

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Bibliographic Details
Published in:Pharmaceutical development and technology 2015-03, Vol.20 (2), p.169-175
Main Authors: Sammeta, Srinivasa M., Wang, Li, Mutyam, Shravan K., O'Loughlin, Kathleen, Green, Carol E., Werner, Milton H., Kelly, Terence, Shankar, Gita N.
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Antiviral Agents - administration & dosage
Antiviral Agents - blood
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
Bioavailability
Biological Availability
co-solvents
cyclodextrins
Drug Delivery Systems
Drug Design
Excipients - chemistry
Humans
Influenza, Human - drug therapy
Intestinal Absorption
Male
Noscapine - administration & dosage
Noscapine - blood
Noscapine - chemistry
Noscapine - pharmacology
Rats, Sprague-Dawley
Solubility
Solvents - chemistry
Ussing chambers
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Summary:Abstract 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.
ISSN:1083-7450
1097-9867
DOI:10.3109/10837450.2013.852574