Development of mucoadhesive drug delivery systems by precipitation of chitosan on drug-loaded microparticles

Multiparticulate dosage forms consist of small sub-units containing the drug and having the advantage of more uniform and predictable transit time, better distribution and less local irritation in the gastrointestinal tract, compared to single unit dosage forms [1, 2]. These multiparticulates, when designed as mucoadhesive formulations, can potentially prolong and normalize the residence time in the gastrointestinal tract, and increase oral drug bioavailability due to their adhesive interactions with the gastrointestinal mucus [3]. Examples of methods for preparation of mucoadhesive pellets and microspheres are extrusion–spheronization [1], spray-drying [4], and emulsion-solvent evaporation [5]. Here, we introduce the use of a novel excipient based on calcium carbonate (FCC, Omyapharm) as a drug carrier and adsorption platform of chitosan. FCC has a small particle size (5-15 μm) and a high porosity (70%, v/v), and can be loaded with various drugs by solvent evaporation [6]. Among other polymers, chitosan is well known for its good mucoadhesive properties [7]. Precipitation of chitosan on calcium carbonate templates for the preparation of hollow microcapsules was recently described [8], but not intended to be used as mucoadhesive multiparticulates in order to increase residence time in the human gastrointestinal tract. Furthermore, the dissolution of the calcium carbonate core is not intended in the approach here presented.

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Development of mucoadhesive drug delivery systems by precipitation of chitosan on drug-loaded microparticles
D. Preisig1, M. Weingartner1, F. Varum2, R. Bravo2, R. Alles, J. Huwyler1, M. Puchkov1
1 Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland 2 Tillotts Pharma AG, Rheinfelden, Switzerland
Poster Drug Delivery Reims, 2015
poster_preisigd_reims_april_2015.pdf
Adobe Acrobat Document 1.2 MB