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Please use this identifier to cite or link to this item: http://hdl.handle.net/1942/9913

Title: Effect on the nasal bioavailability of co-processing drug and bioadhesive carrier via spray-drying
Authors: Coucke, D.
Vervaet, C.
Foreman, P.
ADRIAENSENS, Peter
CARLEER, Robert
Remon, J. P.
Issue Date: 2009
Publisher: ELSEVIER SCIENCE BV
Citation: INTERNATIONAL JOURNAL OF PHARMACEUTICS, 379(1). p. 67-71
Abstract: A mucoadhesive combination of a maize starch (Amioca(R), mainly consisting of amylopectine) and a cross-linked acrylic acid-based polymer (Carbopol(R) 974P) was spray-dried with metoprolol tartrate (used as model molecule) in order to develop a powder suitable for nasal drug delivery via a one-step manufacturing process. The bioavailability of metoprolol tartrate after nasal administration of this powder to rabbits was compared with powders manufactured via other procedures: (a) freeze-drying of a dispersion prepared using the co-spray-dried powder, (b) freeze-drying of a dispersion prepared using a physical mixture of drug and mucoadhesive polymers. After co-processing via spray-drying a low bioavailability (BA 10.8 +/- 2.3%) was obtained, whereas manufacturing procedures based on freeze-drying yielded a higher BA: 37.9 +/- 12.8% using the co-processed powder and 73.6 +/- 24.9% using the physical mixture. The higher bioavailability was due to the deprotonation of poly(acrylic acid) during neutralisation of the dispersion prior to freeze-drying. This induced repulsion of the ionised carboxyl groups and a lower interaction between poly(acrylic acid) and starch, creating a less compact matrix upon hydration of the polymer and allowing an easier escape of metoprolol tartrate from the matrix. This study showed that co-processing of a mucoadhesive Amioca(R)/Carbopol(R) 974P formulation with metoprolol tartrate via co-spray-drying did not provide any added value towards the bioavailability of the drug after nasal administration of the mucoadhesive powder. (C) 2009 Elsevier B.V. All rights reserved.
Notes: [Coucke, D.; Vervaet, C.; Remon, J. P.] Univ Ghent, Pharmaceut Technol Lab, B-9000 Ghent, Belgium. [Adriaensens, P.; Carleer, R.] Hasselt Univ, Div Chem, Inst Mat Res IMO, Hasselt, Belgium.
URI: http://hdl.handle.net/1942/9913
DOI: 10.1016/j.ijpharm.2009.06.008
ISI #: 000269809600009
ISSN: 0378-5173
Category: A1
Type: Journal Contribution
Validation: ecoom, 2010
Appears in Collections: Research publications

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