ORBi: Evrard Brigitte - Contribution of cyclodextrins in the developement of different pharmaceutical formulations of a nex matrix metalloproteinase inhibitor

Reference : Contribution of cyclodextrins in the developement of different pharmaceutical formulatio...


	Document type :	Scientific journals : Article
	Discipline(s) :	Human health sciences : Pharmacy, pharmacology & toxicology
	To cite this reference:	http://hdl.handle.net/2268/73286

Title :	Contribution of cyclodextrins in the developement of different pharmaceutical formulations of a nex matrix metalloproteinase inhibitor
Language :	English
Author, co-author :	Evrard, Brigitte [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
	Bertholet, Pascal [> >]
	Guéders, Maud [Université de Liège - ULg > Département des sciences cliniques > Labo de biologie des tumeurs et du développement >]
	Piette, Marie [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
	Piel, Géraldine [Université de Liège - ULg > Département de pharmacie > Pharmacie galénique >]
	Cataldo, Didier [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Biochimie et physiologie générales, humaines et path. >]
	Delattre, Luc [Université de Liège - ULg > Département de pharmacie > Département de pharmacie >]
Publication date :	2007
Journal title :	Journal of Inclusion Phenomena and Molecular Recognition in Chemistry
Publisher :	Springer
Audience :	International
ISSN :	0923-0750
City :	Dordrecht
Country :	Netherlands
Keywords :	[en] matrix metalloproteases ; cyclodextrins ; inhibitro
Abstract :	[en] Ro 28-2653 is a new synthetic inhibitor of matrix metalloproteinases. The ability of these enzymes to degrade various components of the extracellular matrix seems to play a major role in tumors progression and is potentially effective against bronchial remodeling in asthma and BPCO. Ro 28-2653 is very poorly soluble in water. This low solubility estimated at about 0.56 lg/ml in water at 25 C gives rise to difficulties in pharmaceutical formulation of oral, injectable or nebulizable solutions. The purpose of our study is to prepare and to characterize inclusion complexes between Ro 28-2653 and cyclodextrins and to investigate the biopharmaceutical repercussion of the inclusion of the active substance.The complex formation was investigated by phase solubility studies. 1H-NMR spectroscopy and molecular modeling studies were carried out to elucidate the structure of the inclusion complex between Ro 28-2653 and cyclodextrin. Oral, intravenous and nebulizable solutions of Ro 28-2653 were developed with cyclodextrin. The in vivo studies were performed on healthy sheep for the pharmacokinetic evaluation of the oral and intravenous formulations while the nebulization of the complex solution was studied by using an asthma model in mouse.
Target :	Researchers
Permalink :	http://hdl.handle.net/2268/73286

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Open access	Evrard J Incl Phenom Macrocycl Chem 2007.pdf	No commentary	Publisher postprint	187.44 kB	View/Open

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