Aimed to formulate, optimize (using CCD design) and characterize PLGA-CS-Tween 80 nanoparticles, of the drug Rivastigmine Tartrate (RT), for the treatment of Alzheimer’s disease (AD). The pharmacodynamics performance of the nanoparticles (NPs) were evaluated for brain targeting and memory improvement in Aluminium chloride treated model using Morris water maze test and AchE activity analysis. PLGA-CS-Tween 80 nanoparticles prepared with emulsification-solvent evaporation method. Effect of important factors on the particle size, polydispersity, entrapment efficiency and in vitro drug release was studied using CCD design. Prepared nanoparticles showed particle size 143.0nm, polydispersity 0.164, entrapment efficiency 79.649% and in vitro drug release 69.30±0.262% (60h). FTIR studies showed there was no interaction between drug and polymers. DSC studies indicated that RT was evenly dispersed as amorphous form into NPs. SEM studies indicated that the NPs were spherical in shape and rough at surface. The stability study for six months demonstrated that the formulations were stable at refrigerator (3-5°C) condition is most suitable for storage of nanoparticles. In vivo behavioral study and AchE activity analysis demonstrated that, the rats treated with NPs showed markedly better memory retention compare to pure drug treatment. The study demonstrated that successful targeting of RT, to the brain by chitosan (CS) and Tween 80 coated NPs, have significant therapeutic potential to treat AD and potential carrier for providing sustained brain delivery of RT.
