Pharmaceutical research · 2008
Solid lipid nanoparticles as delivery systems for bromocriptine.
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Esposito Elisabetta, Fantin Martina, Marti Matteo, Drechsler Markus, Paccamiccio Lydia, Mariani Paolo, Sivieri Elisa, Lain Francesco, Menegatti Enea, Morari Michele, Cortesi Rita
Аннотация
PURPOSE: The present investigation describes a formulative study for the development of innovative drug delivery systems for bromocriptine.
METHODS: Solid lipid nanoparticles (SLN) based on different lipidic components have been produced and characterized. Morphology and dimensional distribution have been investigated by electron microscopy and Photon Correlation Spectroscopy. The antiparkinsonian activities of free bromocriptine and bromocriptine encapsulated in nanostructured lipid carriers were evaluated in 6-hydroxydopamine hemilesioned rats, a model of Parkinson's disease.
RESULTS: Tristearin/tricaprin mixture resulted in nanostructured lipid carriers with stable mean diameter up to 6 months from production. Bromocriptine was encapsulated with high entrapment efficiency in all of the SLN samples, particularly in the case of tristearin/tricaprin mixture. Bromocriptine encapsulation did not change nanoparticle dimensions. In vitro release kinetics based on a dialysis method demonstrated that bromocriptine was released in a prolonged fashion for 48 h. Tristearin/tricaprin nanoparticles better controlled bromocriptine release. Both free and encapsulated bromocriptine reduced the time spent on the blocks (i.e. attenuated akinesia) in the bar test, although the action of encapsulated bromocriptine was more rapid in onset and prolonged.
CONCLUSIONS: It can be concluded that nanostructured lipid carriers encapsulation may represent an effective strategy to prolong the half-life of bromocriptine.
METHODS: Solid lipid nanoparticles (SLN) based on different lipidic components have been produced and characterized. Morphology and dimensional distribution have been investigated by electron microscopy and Photon Correlation Spectroscopy. The antiparkinsonian activities of free bromocriptine and bromocriptine encapsulated in nanostructured lipid carriers were evaluated in 6-hydroxydopamine hemilesioned rats, a model of Parkinson's disease.
RESULTS: Tristearin/tricaprin mixture resulted in nanostructured lipid carriers with stable mean diameter up to 6 months from production. Bromocriptine was encapsulated with high entrapment efficiency in all of the SLN samples, particularly in the case of tristearin/tricaprin mixture. Bromocriptine encapsulation did not change nanoparticle dimensions. In vitro release kinetics based on a dialysis method demonstrated that bromocriptine was released in a prolonged fashion for 48 h. Tristearin/tricaprin nanoparticles better controlled bromocriptine release. Both free and encapsulated bromocriptine reduced the time spent on the blocks (i.e. attenuated akinesia) in the bar test, although the action of encapsulated bromocriptine was more rapid in onset and prolonged.
CONCLUSIONS: It can be concluded that nanostructured lipid carriers encapsulation may represent an effective strategy to prolong the half-life of bromocriptine.
Предметные рубрики MeSH
Absorptiometry, PhotonAnimalsAntiparkinson AgentsBehavior, AnimalBromocriptineChromatography, High Pressure LiquidCryoelectron MicroscopyDialysisDrug Delivery SystemsKineticsLightLipidsMaleMicroscopy, ElectronNanoparticlesOxidopamineParkinson Disease, SecondaryRatsRats, Sprague-DawleyScattering, RadiationSpectrophotometry, UltravioletTriglyceridesX-Ray Diffraction