FORMULATION AND EVALUATION OF NOVEL BRAIN TARGETING DRUG LOADED IN LIPID-BASED NANOPARTICLES THROUGH INTRANASAL ROUTE FOR ALZHEIMER

Abstract

Objective: Alzheimer's disease is a slowly progressive disease that takes 7 to 10 years from onset to death. Design and development of different lipid- based drug delivery systems (Niosomes) loaded with rivastigmine tartarate is used to solve the problem of the extensive rapid metabolism of rivastigmine. Niosomes as a nanocarriers of rivastigmine will increase its bioavailability and brain targeting. Methods: Niosomes are prepared using Hand Shaking Method (Thin Film Hydration Technique). Span 60 and cholesterol are dissolved in organic mix solvent, until forming clear solution in a round bottom flask. Then, the solvent is evaporated under decreased pressure, temperature and 70 rpm in a rotary evaporator leaving solid surfactant and cholesterol as thin film formed on the wall of the flask. This layer is then rehydrated by using aqueous solution containing drug with continuous shaking which cause swelling of surfactant layer. Swelled amphiphiles eventually fold and form vesicles that could entrap the drug. The Prepared nanoparticles were characterized for pH, particle size, surface morphology, entrapment efficiency and in vitro release study. Results The average particle size was 100.7 nm with polydispersity index of 0.232. The zeta potential of the optimized formulation F2 was determined and found to be -19 mV. Surface properties of the nanoparticles were studied by Transmission electron microscopy (TEM) and nanoparticles found to have smooth surface. The Drug entrapment efficiency was found to be in between 83.5 to 86.53% indicated fairly good drug loading in the formulations indicated increased bioavailability of the drug. optimized formulation F2 showed 60 % drug release in 240 minutes indicate sustained release of drug. Conclusion: Rivastigmine could be prepared as a novel niosomes systems to enhance its bioavailability.