Anti-alzheimer activity of tacrine loaded methoxypoly (Ethylene glycol) poly (caprolactone) nanoparticles

Abstract

Objective: The objective of the study was to study the in vitro cytotoxic effects of amyloid-β (Aβ) in SH-SY5Y cells and in vivo therapeutic efficacy of drug-loaded nanoparticles (TMPCN-3) in mice. Methods: In vitro cytotoxic effects of Aβ in SH-SY5Y cells were carried out using 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay; cellular uptake study was carried using a laser scanning fluorescence microscope. The in vivo therapeutic efficacy of drug loaded nanoparticles, optimized formulation (TMPCN-3) were studied in mice. Animals (n=18) were divided into three different groups each consisting of six animals in each group. Results: Treatment with Aβ-induced cytotoxicity showed a 54% decrease in cell viability. Drug-treated with TMPCN-3 showed greater intracellular accumulation. In the invasive study TMPCN-3 nanoparticles, the SH-SY5Y cells (73%) were decreased when compared to the control cells (91%). In vivo therapeutic efficacy of drug-loaded nanoparticles was studied in mice, Morris water maze task shows polymeric nanoformulations indicates critical change execution (expanded memory maintenance) when contrasted with control, step down condition maintains a considered space from response created by the memory change and polymeric nanoformulations, and after that taken by tacrine and control the quantity of errors are higher. The nanoformulations distributed massive decreasing in acetylcholine esterase level brain homogenate. Conclusion: Tacrine-loaded methoxypoly(ethylene glycol) poly(caprolactone) reveals that the in vitro cell line believes emphasized the reduced risk of tacrine loaded nanoparticles as there is a significant decrease half maximal inhibitory concentration and higher convention of drug in the glial cells and by in vivo reflects was confirmed that nanoformulation indicated improved memory.