Cited by 86Advanced Drug Delivery SystemsDrug Solubulity and Delivery SystemsNanoparticle-Based Drug Delivery

New micelle myricetin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment

Open access
Sun, Fengyuan, Zheng, Zhou, Lan, Jie, Li, Xuefei, Li, Mengshuang, Song, Kaichao, Wu, Xianggen·2019·Drug Delivery

Abstract

Myricetin (Myr) is a naturally occurring flavonoid exhibiting diverse biological and pharmacological properties, but its characteristics such as water insolubility, poor aqueous stability, and poor bioavailability limit its clinical application, including in ophthalmology. To increase its clinical application in ophthalmology, Myr was designed to be encapsulated in a polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer (PVCL-PVA-PEG) polymeric micelles to increases its aqueous solubility, stability, and corneal permeability to promote its efficacy in eye disease treatments. Thus, the Myr micelle ophthalmic solution was prepared and characterized encapsulation efficiency (EE), micelle size, and zeta potential. The chemical stability of Myr and the short-term storage stability of the Myr micelle ophthalmic solution were evaluated, followed by in vitro cytotoxicity and in vivo ocular irritation; in vitro cellular uptake and in vivo corneal permeation; and in vitro antioxidant activity and in vivo anti-inflammatory efficacy were also further evaluated. Myr could be incorporated into micelles with high EE. PVCL-PVA-PEG micelles significantly enhanced Myr’s aqueous solubility and chemical stability. The Myr micelle ophthalmic solution also showed high storage stability. In rabbits, the Myr micelle ophthalmic solution displayed good in vitro cellular tolerance. Remarkable improvements in in vitro cellular uptake and in vivo corneal permeation were also observed in the Myr micelle ophthalmic solution, and significant improvements in the in vitro antioxidant activity and in vivo anti-inflammatory efficacy were also obtained. Overall, these results supported that the Myr micelle ophthalmic solution could be a promising nanomedicine for ocular tissues.

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Crossref · 10.1080/10717544.2019.1622608

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  • Myr micelle ophthalmic solution demonstrated enhancements in cellular uptake and corneal permeation, alongside improvements in antioxidant activity and anti-inflammatory efficacy.

    “The Myr micelle ophthalmic solution demonstrated distinguished enhancements in both cellular uptake and corneal permeation, alongside significant improvements in its antioxidant activity and anti-inflammatory efficacy [120].”

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Authors
Sun, F., Zheng, Z., Lan, J., Li, X., Li, M., Song, K., & Wu, X.
Affiliations
  • Qingdao University of Science and Technology (CN)
  • First Institute of Oceanography (CN)
  • Shandong Eye Institute & Hospital (CN)
Corresponding author
Wu, Xianggen
Venue
Drug Delivery
Published
2019-01-01
Volume
26
Issue
1
Pages
575-585
ISSN
  • 1071-7544 (ISSN-L)
  • 1521-0464
OpenAlex
W2948295497
Cited by
85
References
47
Citations by year
2026: 5 · 2025: 15 · 2024: 10 · 2023: 13 · 2022: 18 · 2021: 9 · 2020: 14 · 2019: 1
FWCI
4.58
Type
journal article
Language
en
Open access
Locations
  • Drug Delivery (publishedVersion, cc-by-nc)
  • Europe PMC (PubMed Central) (publishedVersion, cc-by-nc)
  • PubMed Central (publishedVersion, cc-by-nc)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Keywords
myricetin, polymeric micelles, ocular drug delivery, flavonoids, eye drops, aqueous solubility enhancement, chemical stability, corneal permeation, eye irritation, cytotoxicity, antioxidant activity, anti-inflammatory efficacy, encapsulation efficiency, nanomedicine
MeSH terms
Animals, Anti-Inflammatory Agents, Chemistry, Pharmaceutical, Cornea, Drug Carriers, Flavonoids, Micelles, Ophthalmic Solutions, Permeability, Polyethylene Glycols, Polymers, Polyvinyls, Rabbits, Solubility, Drug Delivery Systems, Administration, Ophthalmic

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