Published: CABEQ 26 (4) (2012) 405–415
Paper type: Original Scientific Paper
I. De Simone, N. Coceani, R. Farra, S. M. Fiorentino, G. Grassi, R. Lapasin, D. Hasa, B. Perissutti, M. Grassi and D. Voinovich
Abstract
One of the possible causes of failure of the mechanochemical activation of poorly
soluble drugs relies on the scarce drug wettability. Indeed, the mechanochemical process comports the disposition of drug nano-crystals and amorphous drug, generated by the destruction of original drug macro-crystals, on the surface of the carrier (acting as stabiliser), usually represented by crosslinked polymeric particles. Accordingly, the scarce drug wettability can reduce the beneficial action of mechanochemical activation (nano-crystals and amorphous drug are characterised by a higher solubility with respect to the original macro-crystals). In this light, this paper is focussed on the use of surfactants for the increase of delivery system (drug plus carrier) wettability. In particular, the surfactant-polymer systems are characterised for what concerns their bulk and surface properties. This allows to select the best surfactant and to experimentally verify its effect on the release kinetics of a poorly soluble and wettable drug.
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Keywords
Wettability, mechanochemical activation, surfactant, surface characterization