Development and characterization of solid lipid nanoparticles as efficient carriers for lipidic drugs against lung adenocarcinoma tumoral cells

ISLAN GA; RODENAK-KLADNIEW B; DE BRAVO MG; DURAN N; CASTRO GR

Rosario

Congreso; Ricifa 2016 - Reunión Internacional de Ciencias Farmacéuticas.; 2016

Universidad Nacional de Rosario

Solid lipid nanoparticles (SLN) with differentcompositions have been developed for an efficient encapsulation of lipophiliccompounds with biological activities in order to improve their bioavailabilityin physiological mediums. Linalool (LN) is a monoterpene found in essentialoils of plants showing antiproliferative activity in cancer cells and proposedas model drug. SLNs composed of lipids with melting points from 41ºC to 53ºC wereprepared by ultrasonication method in presence of Pluronic®F68 assurfactant. The LN encapsulation percentages in SLNs were in the range of 80-90%for the tested formulations and exhibited invitro LN controlled release profiles for 72 h. The nanoparticle´s size,morphology and distribution were determined by dynamic light scattering (DLS) combinedwith transmission electron microscopy (TEM). SLNs displayed spherical shape andmean diameters in the range of 90-130 nm with narrow size dispersion (PDI) lowerthan 0.2 and Z-potentials around -4.0 mV. The loaded nanoparticles were extensivelycharacterized by FTIR, XRD, DSC and TGA and results indicated the presence ofweak interactions between the components that change the thermal and structuralproperties of SLNs. The formulations, and particularly SLN composed of myristylmyristate as lipid matrix, showed invitro antiproliferative effects against lung adenocarcinoma (A549) celllines in a dose/time manner, enhancing the citotoxicity compared with free LN. Inaddition, the cellular uptake of SLN was observed by labeling the SLNs with afluorescent probe, indicating the ability of nanoparticles to enter intotumoral cells and intracellularly deliver the cargo molecules.