Polysaccharide-based aerogel microspheres for oral drug delivery. (6th March 2015)

• Record Type: Journal Article
• Authors: García-González, C.A.; Jin, M.; Gerth, J.; Alvarez-Lorenzo, C.; Smirnova, I.
• Is Part Of: Carbohydrate polymers. Volume 117(2015)
• Page Start: 797
• Page End: 806
• Publication Date: 2015-03-06
• Subjects: Polysaccharide-based aerogel -- Ketoprofen -- Benzoic acid -- Supercritical impregnation -- Drug release kinetics; Polysaccharides -- Periodicals; Polysaccharides -- Periodicals; Polysaccharides -- Périodiques; Electronic journals; 547.78
• DOI: 10.1016/j.carbpol.2014.10.045
• Languages: English
• ISSNs: 0144-8617

Abstract

Graphical abstract: Highlights: Polysaccharide aerogel microspheres are investigated as carriers of drugs for oral administration. Aerogels were loaded with ketoprofen and benzoic acid, poorly water soluble model drugs. Starch, with the lowest specific surface area, was more prone to adsorb drug molecules. Release of ketoprofen from alginate and pectin aerogel particles was sensitive to pH of the medium. Results point out the possibilities of polysaccharide aerogels of tuning drug loading and release. Abstract: Polysaccharide-based aerogels in the form of microspheres were investigated as carriers of poorly water soluble drugs for oral administration. These bio-based carriers may combine the biocompatibility of polysaccharides and the enhanced drug loading capacity of dry aerogels. Aerogel microspheres from starch, pectin and alginate were loaded with ketoprofen (anti-inflammatory drug) and benzoic acid (used in the management of urea cycle disorders) via supercritical CO2 -assisted adsorption. Amount of drug loaded depended on the aerogel matrix structure and composition and reached values up to 1.0 × 10 −3 and 1.7 × 10 −3 g/m 2 for ketoprofen and benzoic acid in starch microspheres. After impregnation, drugs were in the amorphous state in the aerogel microspheres. Release behavior was evaluated in different pH media (pH 1.2 and 6.8). Controlled drug release from pectin and alginate aerogel microspheres fitted Gallagher–Corrigan release model ( R 2 > 0.99 in both cases), with different relative contribution of erosion and diffusion mechanisms depending on the matrix composition. Release from starch aerogel microspheres was driven by dissolution, fitting the first-order kinetics due to the rigid starch aerogel structure, and showed different release rate constant ( k 1 ) depending on the drug (0.075 and 0.160 min −1 for ketoprofen and benzoic acid, respectively). Overall, the results point out the possibilities of tuning drug loading and release by carefully choosing the polysaccharide used to prepare the aerogels.