Intranasal Delivery of Genistein-Loaded Nanoparticles as a Potential Preventive System against Neurodegenerative Disorders
Open accessAbstract
Genistein has been reported to have antioxidant and neuroprotective activity. Despite encouraging in vitro and in vivo results, several disadvantages such as poor water solubility, rapid metabolism, and low oral bioavailability limit the clinical application of genistein. The aim of this study was to design and characterize genistein-loaded chitosan nanoparticles for intranasal drug delivery, prepared by the ionic gelation technique by using sodium hexametaphosphate. Nanoparticles were characterized in vitro and their cytotoxicity was tested on PC12 cells. Genistein-loaded nanoparticles were prepared, and sodium hexametaphosphate was used as a valid alternative to well-known cross-linkers. Nanoparticle characteristics as well as their physical stability were affected by formulation composition and manufacturing. Small (mean diameters of 200–300 nm) and homogeneous nanoparticles were obtained and were able to improve genistein penetration through the nasal mucosa as compared to pure genistein. Nanoparticle dispersions showed a pH consistent with the nasal fluid and preserved PC12 cell vitality.
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Nasal administration of drugs using the nose-to-brain pathway allows direct drug targeting into the brain, avoiding the first-pass effect and bypassing the BBB.
“The nasal administration of drugs using the nose-to-brain pathway allows direct drug targeting into the brain, avoiding the first-pass effect and bypassing the BBB.”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [17]
The Introduction says drugs or particles can reach the brain directly through the olfactory epithelium or trigeminal nerves, supporting direct nose-to-brain targeting and bypass of the BBB. It does not state that nasal delivery avoids the first-pass effect, so that part of the attributed claim is unsupported. (LLM, conf=0.84)
Experimental — accuracy not yet measuredNose-to-brain drug delivery is a painless, non-invasive administration route that can deliver therapeutic agents into the brain by bypassing the blood-brain barrier.
“Nose-to-brain drug delivery is a painless, non-invasive administration route that can be used to deliver therapeutic agents into the brain by bypassing the BBB [10,14,15,16,17].”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [17]
The Introduction (page not provided) describes intranasal delivery as non-invasive and says drugs or particles can reach the brain directly via the olfactory epithelium or trigeminal nerves, supporting the route’s potential to bypass the BBB. It does not describe the route as painless; the Results and Discussion instead discuss the possibility of irritation upon intranasal administration. (LLM, conf=0.86)
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References 61 · Cited by 107
- Authors
- Rassu, G., Porcu, E. P., Fancello, S., Obinu, A., Senes, N., Galleri, G., Migheli, R., Gavini, E., & Giunchedi, P.
- Affiliations
- University of Sassari (IT)
- University of Pavia (IT)
- Corresponding author
- Gavini, Elisabetta
- Venue
- Pharmaceutics
- Publisher
- MDPI AG
- Published
- 2018-12-29
- Volume
- 11
- Issue
- 1
- Pages
- 8
- ISSN
- 1999-4923 (ISSN-L)
- PMC
- PMC6359056
- OpenAlex
- W2907497428
- Cited by
- 107
- References
- 61
- Citations by year
- 2026: 9 · 2025: 12 · 2024: 11 · 2023: 21 · 2022: 10 · 2021: 15 · 2020: 25 · 2019: 4
- FWCI
- 5.16
- Type
- journal article
- Language
- en
- Open access
- gold
- dx.doi.org
- Licence
- Locations
- Pharmaceutics (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, other-oa)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- UnissResearch (Università degli Studi di Sassari) (submittedVersion, cc-by)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
- Keywords
- genistein, chitosan nanoparticles, intranasal drug delivery, ionic gelation, sodium hexametaphosphate, neurodegenerative diseases, neuroprotection, antioxidant activity, PC12 cells, cytotoxicity, nanoparticle stability, bioavailability enhancement
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