Brain-targeted solid lipid nanoparticles containing riluzole: preparation, characterization and biodistribution.
OBJECTIVE
Developments within nanomedicine have revealed a great potential for drug delivery to the brain. In this study nanoparticulate systems as drug carriers for riluzole, with sufficiently high loading capacity and small particle size, were prepared to a reach therapeutic drug level in the brain.


METHODS
Solid lipid nanoparticles containing riluzole have great potential as drug-delivery systems for amyotrophic lateral sclerosis and were produced by using the warm oil-in-water microemulsion technique. The resulting systems obtained were approximately 88 nm in size and negatively charged. Drug-release profiles demonstrated that a drug release was dependent on medium pH. Biodistribution of riluzole blended into solid lipid nanoparticles was carried out after administration to rats and the results were compared with those obtained by riluzole aqueous dispersion administration. Rats were sacrificed at time intervals of 8, 16 and 30 h, and the riluzole concentration in the blood and organs such as the brain, liver, spleen, heart and kidney was determined.


RESULTS
It was demonstrated that these solid lipid nanoparticles were able to successfully carry riluzole into the CNS. Moreover, a low drug biodistribution in organs such as the liver, spleen, heart, kidneys and lung was found when riluzole was administered as drug-loaded solid lipid nanoparticles.


CONCLUSIONS
Riluzole-loaded solid lipid nanoparticles showed colloidal size and high drug loading, a greater efficacy than free riluzole in rats, a higher capability to carry the drug into the brain and a lower indiscriminate biodistribution.
Bondì
Maria Luisa
ML
Istituto per lo Studio dei Materiali Nanostrutturati, sez di Palermo, Consiglio Nazionale delle Ricerche, Via Ugo La Malfa 153, 90146 Palermo, Italy. marialuisa.bondi@ismn.cnr.it
Craparo
Emanuela Fabiola
EF
Giammona
Gaetano
G
Drago
Filippo
F
D000818:Animals; D001921:Brain / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry; D018696:Neuroprotective Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D010316:Particle Size; D010949:Plasma / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D019782:Riluzole / Q000008:administration & dosage* / Q000493:pharmacokinetics*
D004337:Drug Carriers; D008055:Lipids; D018696:Neuroprotective Agents; D019782:Riluzole