Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 496, Issue 2, Pages 360-370Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2015.10.045
Keywords
Supercritical CO2; Hybrid aerogel; Silica; Gelatin; Acid drugs
Categories
Funding
- Generalitat de Catalunya
- Spanish MEC [NASSOS 2014SGR377, CTQ2014-56324]
- European Union
- European Social Fund
- [TAMOP-4.2.2.A-11/1/KONV-2012-0036]
- [TAMOP-4.2.4B/2-11/1-2012-0001]
- [RyC-2012-11588]
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A comprehensive study of 14 hybrid aerogels of different composition with applications in drug delivery has been carried out. The overall objective was to modulate the release behavior of drug-impregnated aerogels, from an almost instantaneous release to a semi-retarded delivery prolonged during several hours, through internal surface functionalization. The designed hybrid aerogels were composed of silica and gelatin and functionalized with either phenyl, long (16) hydrocarbon chain or methyl moiety. As model systems, three class II active agents (pK(a) < 5.5), ibuprofen, ketoprofen and triflusal, were chosen to impregnate the aerogels. The work relied on the use of supercritical fluid technology for both the synthesis and functionalization of the hybrid aerogels, as well as for the impregnation with an active agent using supercritical CO2 as a solvent. For the impregnated aerogels, in vitro release profiles were recorded under gastric and intestinal pH-conditions using HPLC techniques. The release behavior observed for the three studied drugs was explained considering the measured dissolution profiles of the crystalline drugs, the aerogel composition and its functionalization. Such features are considered of great interest to tailor the bioavailability of drugs with low water solubility. (C) 2015 Elsevier B.V. All rights reserved.
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