Solid lipid nanoparticles as delivery systems for bromocriptine.
OBJECTIVE
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.
Esposito
Elisabetta
E
Department of Pharmaceutical Sciences, University of Ferrara, 44100 Ferrara, Italy. ese@unife.it
Fantin
Martina
M
Marti
Matteo
M
Drechsler
Markus
M
Paccamiccio
Lydia
L
Mariani
Paolo
P
Sivieri
Elisa
E
Lain
Francesco
F
Menegatti
Enea
E
Morari
Michele
M
Cortesi
Rita
R
D015502:Absorptiometry, Photon; D000818:Animals; D000978:Antiparkinson Agents / Q000008:administration & dosage* / Q000627:therapeutic use; D001522:Behavior, Animal / Q000187:drug effects; D001971:Bromocriptine / Q000008:administration & dosage* / Q000627:therapeutic use; D002851:Chromatography, High Pressure Liquid; D020285:Cryoelectron Microscopy; D003956:Dialysis; D016503:Drug Delivery Systems; D007700:Kinetics; D008027:Light; D008055:Lipids; D008297:Male; D008854:Microscopy, Electron; D053758:Nanoparticles; D016627:Oxidopamine; D010302:Parkinson Disease, Secondary / Q000139:chemically induced / Q000188:drug therapy; D051381:Rats; D017207:Rats, Sprague-Dawley; D012542:Scattering, Radiation; D013056:Spectrophotometry, Ultraviolet; D014280:Triglycerides; D014961:X-Ray Diffraction
D000978:Antiparkinson Agents; D008055:Lipids; D014280:Triglycerides; D001971:Bromocriptine; D016627:Oxidopamine; C010800:tricaprin; C022618:tristearin