Design, characterization and in vitro evaluation of linalool-loaded solid lipid nanoparticles as potent tool in cancer therapy

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

COLLOIDS AND SURFACES B-BIOINTERFACES

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2017 vol. 154 p. 123 - 132

0927-7765

Linalool(LN) is a monoterpene found in essential oils of plants and herbs producing multipleeffects on the mevalonate pathway and interesting antiproliferative activity incancer cells. However, due to its poor aqueous solubility, an efficient vehicleis needed to improve its administration and bioavailability in physiological mediums. LN encapsulation in solid lipid nanoparticles (SLN) with different compositions hadbeen explored and in vitro tested in twocancer cell lines. SLN of myristyl myristate (MM), cetyl esters (SS) and cetylpalmitate (CP) were prepared by sonication in presence of Pluronic®F68 as surfactant. Nanoparticle´s size, morphology and distribution were determinedby dynamic light scattering in combination with optical and transmission electronmicroscopy (TEM). SLNs showed spherical shape and mean diameters in the rangeof 90-130 nm with narrow size dispersion (PDI values lower than 0.2) and Zpotentials around -4.0 mV. The encapsulation percentages of LN in SLN werehigher than 80% for all tested formulations and exhibited in vitro LN controlled release profiles for at least 72 hours. Thenanoparticles were physicochemical characterized by FTIR, XRD, DSC and TGA and theincorporation of LN into SLN was higher than 80% in tested matrices. Thedeveloped formulations, and in particular SLN (MM)-LN, showed in vitro antiproliferative effects on hepatocarcinoma(HepG2) and lung adenocarcinoma (A549) cell lines in a dose-dependent responseand higher inhibitory effects were found in comparison with free LN. Thecellular uptake of SLN was demonstrated by fluorescence microscopy, enhancingthe ability of nanoparticles to intracellular delivery the cargo molecules.