By a News Reporter-Staff News Editor at Life Science Weekly -- Researchers detail new data in Membrane Proteins. According to news reporting out of Groningen, Netherlands, by NewsRx editors, research stated, "The inclusion of nanoparticles dispersed in a hydrophilic matrix is one of the formulation strategies to improve the bioavailability of orally administered Biopharmaceutics Classification System (BCS) class II and IV drugs by increasing their dissolution rate in the intestine. To confirm that the increased dissolution rate results in increased bioavailability, in vitro and in vivo animal experiments are performed, however, translation to the human situation is hazardous."
Our news journalists obtained a quote from the research from the University of Groningen, "In this study, we used a range of in vitro and ex vivo methods, including methods applying human tissue, to predict the in vivo oral bioavailability of a model BCS class II CB-1 antagonist, formulated as a nanoparticle solid dispersion. The enhanced dissolution rate from the nanoparticle formulation resulted in an increased metabolite formation in both rat and human precision-cut intestinal slices, suggesting increased uptake and intracellular drug concentration in the enterocytes. In Ussing chamber experiments with human tissue, both the metabolite formation and apical efflux of the metabolite were increased for the nanoparticulate solid dispersion compared with a physical mixture, in line with the results in intestinal slices. The pharmacokinetics of the different formulations was studied in rats in vivo. The nanoparticle formulation indeed improved the absorption of the cannabinoid receptor 1 (CB-1) antagonist and the delivery into the brain compared with the physical mixture."
According to the news editors, the research concluded: "The combined approach provides a valuable set of tools to investigate the effects of formulation on the absorption of poorly soluble compounds in human intestine and may provide relevant information on the oral bioavailability in humans early in the development process."
For more information on this research see: Nanoparticle Formulation of a Poorly Soluble Cannabinoid Receptor 1 Antagonist Improves Absorption by Rat and Human Intestine. Drug Metabolism and Disposition, 2013;41(8):1557-1565. Drug Metabolism and Disposition can be contacted at: Amer Soc Pharmacology Experimental Therapeutics, 9650 Rockville Pike, Bethesda, MD 20814-3995, USA (see also Membrane Proteins).
Our news journalists report that additional information may be obtained by contacting S. Siissalo, University of Groningen, Mass Spectrometry Core Facil, Groningen, Netherlands. Additional authors for this research include H. de Waard, M.H. de Jager, R. Hayeshi, H.W. Frijlink, W.L.J. Hinrichs, H. Dinter-Heidorn, A. van Dam, J.H. Proost, G.M.M. Groothuis and I.A.M. de Graaf.
Keywords for this news article include: Europe, Terpenes, Groningen, Netherlands, Membrane Proteins, Cannabinoid Receptors, G-Protein-Coupled Receptors
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