Rivastigmine nasal spray for the treatment of Alzheimer’s Disease: Olfactory deposition and brain delivery
Abstract
Alzheimer's disease (AD) is characterized by a gradual decline in cognitive function and memory impairment, significantly impacting the daily lives of patients. Rivastigmine (RHT), a cholinesterase inhibitor, is used to treat mild to moderate AD via oral administration. However, oral administration is associated with slow absorption rate and severe systemic side effects. RHT nasal spray (RHT-ns), as a nose-to-brain delivery system, is more promising for AD management due to its efficient brain delivery and reduced peripheral exposure. This study constructed RHT-ns for enhancing AD treatment efficacy, and meanwhile the correlation between drug olfactory deposition and drug entering into the brain was explored. A 3D-printed nasal cast was employed to quantify the drug olfactory deposition. Brain delivery of RHT-ns was quantified using fluorescence tracking and Desorption Electrospray Ionization Mass Spectrometry (DESI-MS) analysis, which showed a good correlation to the olfactory deposition. F 2 (containing 1% (w/v) viscosity modifier Avicel® RC-591) with high olfactory deposition and drug brain delivery was further investigated for pharmacodynamics study. F 2 exhibited superiority in AD treatment over the commercially available oral formulation. In summary, the present study showed the successful development of RHT-ns with improved olfactory deposition and enhanced brain delivery. It might provide new insight into the design and development of nose-to-brain systems for the treatment of AD.
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Compared to oral pills, transdermal patches are more pleasant and provide a smaller dosage, leading to fewer side effects.
“Compared to oral pills, transdermal patches are more pleasant and provide a smaller dosage, which leads to fewer side effects.”
From Recent Advances in Therapeutics for the Treatment of Alzheimer’s Disease (2024) · cites this paper as [120]
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- Authors
- Guo, H., Wang, G., Zhai, Z., Huang, J., Huang, Z., Zhou, Y., Xia, X., Yao, Z., Huang, Y., Zhao, Z., Wu, C., & Zhang, X.
- Affiliations
- Guangdong University of Technology (CN)
- Sun Yat-sen University (CN)
- Jinan University (CN)
- Corresponding author
- Huang, Jiayuan
- Huang, Zhengwei
- Huang, Ying
- Zhao, Ziyu
- Zhang, Xuejuan
- ORCID
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2024-03
- Volume
- 652
- Pages
- 123809
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W4390837736
- Cited by
- 31
- References
- 34
- Citations by year
- 2026: 11 · 2025: 12 · 2024: 8
- FWCI
- 5.40
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Fundamental Research Funds for the Central Universities (21621014)
- National Natural Science Foundation of China (82104072)
- Guangzhou Municipal Science and Technology Project (202201010424)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
- Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
- Keywords
- rivastigmine, nasal spray, Alzheimer's disease, nose-to-brain delivery, brain drug delivery, cholinesterase inhibitors, desorption electrospray ionization mass spectrometry, fluorescence tracking, pharmacodynamics
- MeSH terms
- Rivastigmine, Administration, Intranasal, Alzheimer Disease, Brain, Cholinesterase Inhibitors, Humans, Nasal Sprays
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