Design and development of donepezil hydrochloride loaded nanostructured lipid carriers for efficient management of Alzheimer’s disease

Objective

The primary objective of this study was to develop nanostructured lipid carriers of donepezil hydrochloride (DNZ HCl) for effective management of Alzheimer’s disease (AD).

Significance

Intranasal administration of DNZ NLC containing Nigella sativa (NS) oil as a liquid lipid may significantly improve nasal penetration and deliver the drug directly to the brain avoiding blood brain barrier (BBB).

Method

High pressure homogenization was used to prepare nanostructured lipid carriers (NLCs), followed by ultrasonication. Glyceryl monostearate (GMS), Tween 80, and Poloxamer 407 were used as solid lipid, surfactant and co-surfactant respectively, whereas, Nigella sativa oil was used as a liquid lipid.

Result

The particle size, polydispersity index and zeta potential were found to be 107.4 ± 2.64 nm, 0.25 ± 0.04 and −41.7 mV. The entrapment efficiency and drug content were found to be 70.20% and 89.05% respectively. After intranasal administration of Donepezil hydrochloride (DNZ HCl) loaded NLC’s, the maximum concentrations (C_max) of 4.597 µg/mL in brain and 2.2583 µg/mL in blood was achieved after 1 h (T_max).

Conclusion

The formulated DNZ HCl loaded NLCs significantly improved nasal penetration and enhanced drug distribution in brain resulting in a potentially effective intranasal drug delivery system for the effective management of Alzheimer’s disease.

Read more

Avinash R. Tekade, Mayuri R. Suryavanshi, Ashutosh B. Shewale & Vilas S. Patil (2023) Design and development of donepezil hydrochloride loaded nanostructured lipid carriers for efficient management of Alzheimer’s disease, Drug Development and Industrial Pharmacy,
DOI: 10.1080/03639045.2023.2262035