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Characterization and in vivo evaluation of ketotifen-loaded chitosan microspheres

机译:Characterization and in vivo evaluation of ketotifen-loaded chitosan microspheres

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摘要

Ketotifen (KT)-loaded chitosan microspheres (MS) were prepared for controlled release of the antihista-minic drug, and their use as delivery systems in the intraperitoneal cavity of rats was investigated. Microspheres were prepared by a spray-drying method followed by treating with glutaraldehyde solutions in methanol as cross-linker. Results showed that very small spherical microspheres (1.0-1.3 μm) with a high load of KT (92 ± 6 μg KT/mg) were obtained. KT loading decreased with cross-linking (52 ± 2-46 ± 7μg KT/mg). Interactions between KT and chitosan avoided total KT release from cross-linked MS. After intraperitoneal (i.p.) administration, microsphere aggregations were adhered to muscle subjacent to the tegument and to adipose tissue, and there were no evident sings of rejection; KT was detected in blood stream (0.37-0.25 μg/mL) at 24 h, which was longer than the i.p. administration of the drug in solution (39.4 μg/mL at 2.4 h).

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