Development of an optimized hyaluronic acid-based lipidic nanoemulsion co-encapsulating two polyphenols for nose to brain delivery
Open accessAbstract
The development of mucoadhesive lipidic nanoemulsion based on hyaluronic acid, co-encapsulating two polyphenols (resveratrol and curcumin) for the transnasal treatment of neurodegenerative diseases was attempted in the current manuscript. Nanoemulsions were prepared by the spontaneous emulsification method, and were characterized for their particle size, zeta potential, mucoadhesive strength and morphology. The selected formula was tested for its antioxidant potential, in vitro and ex vivo release of the two polyphenols, safety on nasal mucosa and in vivo quantification of the two drugs in rat brains. Its stability was tested by monitoring the change in particle size, zeta potential, drugs' content and antioxidant potential upon storage for 3 months. The optimized hyaluronic acid based nanoemulsion formula displayed a particle size of 115.2 ± 0.15 and a zeta potential of -23.9 ± 1.7. The formula displayed a spherical morphology and significantly higher mucoadhesive strength compared to its non mucoadhesive counterpart. In addition, the nanoemulsion was able to preserve the antioxidant ability of the two polyphenols and protect them from degradation. Diffusion controlled release of the two drugs was achievable till 6 hours, with an ex vivo flux across sheep nasal mucosa of 2.86 and 2.09 µg/cm(2)hr for resveratrol and curcumin, respectively. Moreover, the mucoadhesive nanoemulsion was safe on nasal mucosa and managed to increase the amounts of the two polypehnols in the brain (about 7 and 9 folds increase in AUC0-7 h for resveratrol and curcumin, respectively). Hyaluronic acid based lipidic nanoemulsion proved itself as a successful carrier enhancing the solubility, stability and brain targetability of polyphenols.
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In vivo quantification in rat brains showed an increase of the amounts of resveratrol and curcumin in the brain with nanoemulsions compared to solutions.
“In vivo quantification of the two drugs in rat brains showed an increase of the amounts of the two polyphenols in the brain with respect to the administration of solutions.”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [60]
Nanoemulsions can protect loaded drugs from degradation and preserve their antioxidant properties.
“This work is a good example of the use of NEs as formulations that are able to protect loaded drugs from degradation and preserve their antioxidant properties.”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [60]
Diffusion of resveratrol and curcumin across freshly isolated sheep nasal mucosa was achievable for 6 hours.
“Ex vivo flux across freshly isolated sheep nasal mucosa was studied, and diffusion of the two drugs was achievable for 6 hours.”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [60]
Nanoemulsions can load two drugs together.
“Furthermore, this work demonstrates the capability of NEs for loading two drugs together.”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [60]
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“8 Biodistribution (ex vivo and in vivo models) [117]”
Background
- Authors
- Nasr, M.
- Affiliations
- Ain Shams University (EG)
- Corresponding author
- Nasr, Maha
- ORCID
- Nasr, Maha
- Venue
- Drug Delivery
- Publisher
- Informa UK Limited
- Published
- 2015-09-24
- Volume
- 23
- Issue
- 4
- Pages
- 1444-1452
- ISSN
- 1071-7544 (ISSN-L)
- 1521-0464
- OpenAlex
- W1808127154
- Cited by
- 208
- References
- 48
- Citations by year
- 2026: 11 · 2025: 17 · 2024: 27 · 2023: 23 · 2022: 26 · 2021: 24 · 2020: 34 · 2019: 22 · 2018: 12 · 2017: 9 · 2016: 3
- FWCI
- 4.47
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Drug Delivery (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Cairo University
- Faculty of Veterinary Medicine, Cairo University
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- hyaluronic acid, mucoadhesion, nose-to-brain delivery, intranasal drug delivery, resveratrol, curcumin, polyphenols, neurodegenerative diseases, nasal mucosa, drug release, brain drug concentration, antioxidant activity, nanoemulsion stability
- MeSH terms
- Resveratrol, Administration, Intranasal, Animals, Brain, Curcumin, Emulsions, Hyaluronic Acid, Lipids, Nasal Mucosa, Sheep, Stilbenes, Neurodegenerative Diseases, Rats, Nanoparticles, Polyphenols
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