Producción CyT
Medicina (Buenos Aires) - DEVELOPMENT AND IN VITRO CHARACTERIZATION OF NANOSTRUCTURED LIPID CARRIERS LOADING WITH CANNABIDIOL AND STIRIPENTOL AS A POTENTIAL THERAPEUTIC STRATEGY FOR DRAVET SYNDROME
Congreso
Autoría:
SCIOLI MONTOTO, SEBASTIÁN ; Lobos, Eduardo Martín ; Chain, C.Y. ; Islan, German Abel ; Talevi, Alan ; Ruiz, Maria EsperanzaFecha:
2024Editorial y Lugar de Edición:
Fundación Revista MedicinaISSN:
1669-9106Resumen *
Dravet syndrome is a severe drug-resistance type of epilepsy thatcan occur in the first year of life in previously healthy children. Oneof the main problems in the treatment of this syndrome is that drugsacting on sodium channels (phenytoin, carbamazepine, oxcarbazepine,lamotrigine, etc.) cannot be used since they exacerbateseizures in these patients. Recently, only Stiripentol (STP) hasemerged as a specific treatment for this syndrome. However, it hasa very low and variable bioavailability, and a high plasma proteinbinding which could lead to interactions. In recent years cannabidiol(CBD) has shown certain effectivity over refractory epilepsy. Nevertheless,CBD has a low water solubility, low bioavailability and avariable pharmacokinetic, needing high doses to achieve a therapeuticeffect. A strategy capable of overcoming both drugs problemsis their incorporation within nanostructured lipid carriers, capable ofcrossing different biological barriers and thus allowing a better arrivalof these drugs to their site of action, improving their bioavailabilityand decreasing their adverse effects. The objectives of this workwere to develop and characterize, in terms of particle size, Z potential,polydispersity index (PdI) and percentual entrapment efficiency(%EE), nanostructured lipid carriers containing STP and CBD and tostudy their release kinetics. Nanoparticles were prepared using homogenizationby ultrasonication technique. Particle size, Z potentialand PdI were measured using a Z-sizer, while in vitro release studywas carried out by the dialysis bag method. The developed formulationaveraged particle sizes, PdI and Z potential between 174 to 190nm, 0.184 to 0.250 and -11.63 to -6.60 mV, respectively and alsoshowed a high %EE (over 99%). On the other side, drugs showed aprolonged release for up to 24 hs. Although many more studies areneeded, these nanoparticles containing STP and CBD are a promisingtool for the treatment of Dravet syndrome. Información suministrada por el agente en SIGEVAPalabras Clave
STIRIPENTOLCANNABIDIOLDRAVET SYNDROMEEPILEPSYDRUG DELIVERY