Novel spray-dried genipin-crosslinked casein nanoparticles for prolonged release of alfuzosin hydrochloride

Purpose: To propose a simple method for the development of genipin-crosslinked casein micelles as a new delivery platform for prolonged release of alfuzosin hydrochloride. Methods: Crosslinked casein micelles entrapping alfuzosin were transformed into solid redispersible nanoparticles via spray-drying technique with no need for drying adjuvants based on the stabilizing effect of casein. Results: The nanoparticles displayed high production yields (86.99-94.63% w/w) with a reasonable drug incorporation efficiency ranged from 92.86 to 97.75%. The nanoparticles were readily reconstituted in aqueous solution with a particle size range of 122.1-260.0 nm and a zeta potential range of -21.6 to -36.6 mV indicating a good colloidal stability. No drug crystals were detectable in the scanning electron micrographs revealing successful encapsulation of alfuzosin into casein nanoparticles which was confirmed by differential scanning calorimetry. The nanoparticles succeeded in prolonging the drug release that could be controlled by modulating the genipin crosslinking degree. The release data showed a good fit into Higuchi release kinetics with non-Fickian type of drug diffusion. Conclusions: These results demonstrated that genipin-crosslinking combined with spray-drying technique could be used as a promising tool to develop solid redispersible casein nanoparticles with sustained drug release properties. © 2012 Springer Science+Business Media New York.