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

B. RODENAK KLADNIEW; J. S. CISNEROS; CECILIA Y. CHAIN; MARÍA E. VELA; G. R. CASTRO; MARGARITA M. GARCÍA DE BRAVO; G. A. ISLÁN

Congreso; ANNUAL MEETING OF BIOSCIENCE SOCIETIES 2021; 2021

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 wasthe design of biocompatible and non-toxic hybrid pectin (P) nanostructuredlipid carriers (NLC) containing geraniol (GOH), a monoterpenewith antitumor activity, as a novel platform for the bioactivedelivery of anticancer drugs.Nanoparticles (NPs) were prepared by hot homogenization/ultrasonicationmethod. Different pectin formulations were prepared bymodifying their amount (0.1 and 0.5%, w/v) in the formulation and/ormetoxilation degree -Low (LMP, 33%) and high (HMP, 74%). Ten differentformulations were prepared: NLC/GOH, NLC/LMP0.1/GOH,NLC/LMP0.5/GOH, NLC/HMP0.1/GOH, NLC/HMP0.5/GOH, andtheir respective counterparts without GOH. NPs were characterizedby TEM microscopy and DLS: particle size, z-potential (z-pot), andpolydispersity index (PI). The encapsulation efficiency (EE) was determinedby UV-Vis spectroscopy. Cell viability (MTT) and mitochondrialmembrane potential (MMP, fluorescence spectroscopy) in humanlung adenocarcinoma A549 cells were evaluated. NPs showedspherical 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-loadedNLC decreased cell viability up to 10-fold compared to free GOH(GOH 1.5 mM, 24 h, p< 0.001). In addition, GOH-loaded NLCstrongly decreased (p< 0.001) MMP (50 to 94%) in comparison withfree GOH (37%) in A549 cells. These results suggest that hybridNLC/P nanoparticles containing GOH are promising bioactive andinnovative systems for targeted delivery of antineoplastic drugs totreat lung cancer.