Polysaccharide-based aerogel microspheres for oral drug delivery

Journal
Carbohydrate polymers  
Volume
117
Start Page
797
End Page
806
Citation
Carbohydrate Polymers (117): 797-806 (2015-03-06)
Publisher DOI
10.1016/j.carbpol.2014.10.045
Scopus ID
2-s2.0-84915757289
Publisher
Elsevier Science
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/m2 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 (R2 > 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 (k1) 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.
Subjects
Benzoic acid
Drug release kinetics
Ketoprofen
Polysaccharide-based aerogel
Supercritical impregnation
DDC Class
500: Naturwissenschaften
600: Technik
More Funding Information
Spanish Ministry of Science and Innovation (MICINN, Spain) for the financial support through the Juan de la Cierva Fellowship Programme (grant no. JCI-2012-12705 ). The work was partially funded by the Spanish Government (MICINN, Spain, SAF2011-22771 ) and the European Commission (FEDER funds).