Characterization of DG4.0/DG4.5-Tacrine/Carbamazepine Complexes for Alzheimer´s Treatment

IGARTÚA, DE; MARTINEZ, CS; ALONSO, SDV; PRIETO, MJ.

Tucuman

Congreso; III Latin American Federation of Biophysical Societies (LAFeBS) ? IX IberoAmerican Congress of Biophysics ? XLV Reunion Anual SAB; 2016

SAB

Alzheimer's disease is a multifactorial neurodegenerative disease. The most accepted etiological hypotheses are related to a deficiency ofacetylcholine and the formation of senile plaques of β-amyloid protein (Aβ) and neurofibrillary of hyperphosphorylated TAU protein (p-TAU). Tacrine (TAC) is an inhibitor of the enzyme acetylcholinesterase, which was approved by FDA for Alzheimer´s treatment. Due totheir hepatotoxicity, TAC was removed from the market. In contrast, carbamazepine (CBZ) is an antiepileptic drug currently on use thatwas shown to reduce levels of Aβ and p-TAU. However, it has low solubility in aqueous media and inefficient pharmacokinetic profiles.Dendrimers (D) PAMAM DG4.0 and DG4.5 are three-dimensional polymers that bring unique properties to the field of drugs deliverysystems. The complexed drugs assimilate D properties, which would increase significantly their solubility and brain arrival.Therefore, ours aims were to obtain and characterize complexes of DG4.0 or DG4.5 with TAC or CBZ.