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Authors & Affiliations
Alvaro Barrera-Ocampo, Andres Camilo Arana Linares, Paola Andrea Caicedo Burbano, Natalie Charlotte Cortés Rendón, Edison Humberto Osorio López, María Francisca Villegas Torres, Andrés Fernando González Barrios
Abstract
The delivery of molecules like galantamine and DNA aptamers to the brain for the treatment of neurodegenerative diseases is a great challenge because of the blood-brain barrier selectivity. However, nanoliposomal systems can provide an alternative to this drawback. This study aimed to design and develop nanoliposomes based on soy lecithin loaded with galantamine (acetylcholinesterase inhibitor) or DNA aptamers designed to hinder the aggregation of proteins like Aβ, TDP-43 and α-synuclein. For this, a complete physicochemical characterization of soy lecithin and other raw materials was carried out (Lipidomic analysis, IR and DSC). Two formulations were developed, but the one made of soy lecithin, phospholipon® G90 and cholesterol showed the best physicochemical characteristics. This formulation had an average particle size of 150 nm, an average polydispersity index of 0.4 and a Z potential of -40. The encapsulation and release percentages were 70% and 50%, respectively. These values were kept constant during the stability tests at 4°C and 40°C with a relative humidity of 80%. Neither hemolysis nor cytotoxicity was observed during the in vitro assays when liposomes were applied to primary cultures of rat cortical and hippocampal neurons. In vitro release assays evidenced that the liposome formulation was able to deliver galantamine and DNA aptamers across the cell membrane into to the intracellular space of neurons in culture. In conclusion, the nanoliposome formulation obtained in this study may be the basis for the effective delivery to the brain of small organic molecules and biomolecules with pharmacotherapeutic potential for neurodegenerative diseases.