CHARACTERIZATION AND IN VITRO EFFECTS OF GERANIOL-LOADED PECTIN MODIFIED NANOSTRUCTURED LIPID CARRIERS ON LUNG CANCER CELLS

RODENAK-KLADNIEW, BORIS; CISNEROS, JOSÉ SEBASTIÁN; CHAIN, CECILIA YAMIL; VELA, MARÍA E.; CASTRO, GUILLERMO RAUL; DE BRAVO, MARGARITA GARCÍA; ISLAN, GERMAN A

Encuentro; LXVI ANNUAL MEETING OF SOCIEDAD ARGENTINA DE INVESTIGACIÓN CLÍNICA (SAIC); 2021

SAIC . SAI . AAFE . NANOMED.ar

Lung cancer is the first cause of cancer-related deaths in the world. Many of the current therapies are still inefficient and/or present highlytoxic undesirable side effects. The aim of the present work was the design of biocompatible and non-toxic hybrid pectin (P) nanostructuredlipid carriers (NLC) containing geraniol (GOH), a monoterpene with antitumor activity, as a novel platform for the bioactive delivery of anticancer drugs. Nanoparticles (NPs) were prepared by hot homogenization/ultrasonication method. Different pectin formulations were prepared by modifying their amount (0.1 and 0.5%, w/v) in the formulation and/or metoxilation degree -Low (LMP, 33%) and high (HMP, 74%). Ten different formulations were prepared: NLC/GOH, NLC/LMP0.1/GOH, NLC/LMP0.5/GOH, NLC/HMP0.1/GOH, NLC/HMP0.5/GOH, and their respective counterparts without GOH. NPs were characterized by TEM microscopy and DLS: particle size, z-potential (z-pot), and polydispersity index (PI). The encapsulation efficiency (EE) was determined by UV-Vis spectroscopy. Cell viability (MTT) and mitochondrial membrane potential (MMP, fluorescence spectroscopy) in human lung adenocarcinoma A549 cells were evaluated. NPs showed spherical shape, sizes in the range of 110-180 nm with narrow distribution (PI< 0.3), and negative z-pot ranging from -10 to -19 mV. The EE of GOH was higher than 89% in five formulations. GOH-loaded NLC inhibited A549 cell viability in a dose (0.25- 2.00 mM) and time (24 and 72 h) dependent manner. GOH-loaded NLC decreased cell viability up to 10-fold compared to free GOH (GOH 1.5 mM, 24 h, p< 0.001). In addition, GOH-loaded NLC strongly decreased (p< 0.001) MMP (50 to 94%) in comparison with free GOH (37%) in A549 cells. These results suggest that hybrid NLC/P nanoparticles containing GOH are promising bioactive and innovative systems for targeted delivery of antineoplastic drugs to treat lung cancer.