Nanostructured Lipid Carriers of Donepezil Hydrochloride for the Treatment of Alzheimer’s Disease

Title:Nanostructured Lipid Carriers of Donepezil Hydrochloride for the Treatment of Alzheimer’s Disease

Volume: 21

Author(s): Avinash Tekade*, Ram Susar, Gajanan Kulkarni, Samiksha Surwade and Anil Gaikwad

Affiliation:

• Department of Pharmaceutics, Marathwada Mitra Mandal’s College of Pharmacy, Thergaon (Kalewadi), Pune-411033 (M.S.), India

Keywords: Alzheimer’s disease, nanostructured lipid carriers, donepezil hydrochloride, argan oil, nose to brain delivery

Abstract: Background: Alzheimer's Disease (AD) is a long-term brain disorder that worsens over time. A cholinesterase inhibitor called Donepezil HCl (DNZ) is used to treat and control AD. Due to its failure to reach the appropriate concentration in the brain cells, its efficacy upon oral administration is limited, and thus investigation of alternative administration route is necessary.

Objective: The objective of this study was to develop donepezil HCl-loaded Nanostructured Lipid Carriers (NLCs) that can bypass the blood-brain barrier and thus be directly delivered to the brain through the nasal route. This method improves availability at the site of action, reduces the negative effects of oral medication, and ensures an expedited commencement of action.

Method: High-pressure homogenization and ultrasonication were used to formulate NLCs. Glyceryl Monostearate (GMS) as a solid lipid, Tween 80 as a surfactant, and Poloxamer 407 as a co-- surfactant were used. In this study, argan oil was employed as a liquid lipid as well as a penetration enhancer.

Results: The chosen NLCs displayed a particle size of 137.34 ± 0.79 nm, a PDI of 0.365 ± 0.03, and a zeta potential of -10.4 mV. The selected formulation showed an entrapment efficiency of 84.05 ± 1.30% and a drug content of 77.02 ± 0.23%. The concentration of the drug in the brain after intravenous and intranasal administration of DNZ NLCs at 1 h was found to be 0.490 ± 0.007 and 4.287 ± 0.115, respectively. Thus, the concentration of DNZ achieved in the brain after intranasal administration of DNZ NLCs was approximately 9 times more than the concentration when administered by intravenous route.

Conclusion: The DNZ-loaded NLCs, when administered via nasal route, showed markedly improved drug availability in the brain, suggesting an efficient drug delivery strategy to treat Alzheimer's disease.

Cite this article as:

Tekade Avinash*, Susar Ram, Kulkarni Gajanan, Surwade Samiksha and Gaikwad Anil, Nanostructured Lipid Carriers of Donepezil Hydrochloride for the Treatment of Alzheimer’s Disease, Current Alzheimer Research 2024; 21 () . https://dx.doi.org/10.2174/0115672050288659240229080535

DOI https://dx.doi.org/10.2174/0115672050288659240229080535	Print ISSN 1567-2050
Publisher Name Bentham Science Publisher	Online ISSN 1875-5828