title: Nanoparticulate lipid dispersions for bromocriptine delivery: characterization and in vivo study.
abstract: The physico-chemical properties and in vivo efficacies of two nanoparticulate systems delivering the antiparkinsonian drug bromocriptine (BC) were compared in the present study. Monoolein Aqueous Dispersions (MADs) and Nanostructured Lipid Carriers (NLCs) were produced and characterized. Cryogenic transmission electron microscopy (cryo-TEM) and X-ray diffraction revealed the morphology of MAD and NLC. Dimensional distribution was determined by Photon Correlation Spectroscopy (PCS) and Sedimentation Field Flow Fractionation (SdFFF). In particular, BC was shown to be encapsulated with high entrapment efficiency both in MAD and in NLC, according to SdFFF combined with HPLC. Two behavioral tests specific for akinesia (bar test) or akinesia/bradykinesia (drag test) were used to compare the effects of the different BC formulations on motor disabilities in 6-hydroxydopamine hemilesioned rats in vivo, a model of Parkinson's disease. Both free BC and BC-NLC reduced the immobility time in the bar test and enhanced the number of steps in the drag test, although the effects of encapsulated BC were longer lasting (5h). Conversely, BC-MAD was ineffective in the bar test and improved stepping activity in the drag test to a much lower degree than those achieved with the other preparations. We conclude that MAD and NLC can encapsulate BC, although only NLC provide long-lasting therapeutic effects possibly extending BC half-life in vivo.
authors: Department of Pharmaceutical Sciences, University of Ferrara, Ferrara, Italy. ese@unife.it
authors: Elisabetta
authors: E
authors: Esposito
authors: Paolo
authors: P
authors: Mariani
authors: Laura
authors: L
authors: Ravani
authors: Catia
authors: C
authors: Contado
authors: Mattia
authors: M
authors: Volta
authors: Simone
authors: S
authors: Bido
authors: Markus
authors: M
authors: Drechsler
authors: Serena
authors: S
authors: Mazzoni
authors: Enea
authors: E
authors: Menegatti
authors: Michele
authors: M
authors: Morari
authors: Rita
authors: R
authors: Cortesi
mesh_terms: D000818:Animals; D000978:Antiparkinson Agents / Q000008:administration & dosage* / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects; D001971:Bromocriptine / Q000008:administration & dosage* / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D031521:Fractionation, Field Flow; D005989:Glycerides / Q000737:chemistry; D008055:Lipids / Q000737:chemistry; D008297:Male; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D020734:Parkinsonian Disorders / Q000188:drug therapy; D051381:Rats; D017207:Rats, Sprague-Dawley; D013997:Time Factors; D014961:X-Ray Diffraction
chemical_list: D000978:Antiparkinson Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005989:Glycerides; D008055:Lipids; D001971:Bromocriptine; C005953:monoolein