Preparation and in vitro-in vivo evaluation of novel ocular nanomicelle formulation of thymol based on glycyrrhizin
Abstract
The development of an efficient ocular drug delivery system is helpful in improving the ocular diffusion of topically delivered drugs as well as enhancing drugs therapeutic efficacy. The objective of this study was to explore the potential of self-assembled nanomicelles based on glycyrrhizin in ocular topical applications. In brief, a dipotassium glycyrrhizinate (DG)-based nanomicelle ophthalmic solution encapsulating thymol (DG-THY) was developed using a simple thin-film dispersion method. The optimal formulation featured a DG/thymol (THY) weight ratio of 9:1 and an encapsulation efficiency of 98.25 ± 1.16%; the nanomicelles were ultra-small spheres with an average particle size of 3.30 ± 0.39 nm, a polydispersity index of 0.22 ± 0.02, and an electrically negative surface (-[10.03 ± 1.31] mV) for the optimized DG-THY. This DG-THY ophthalmic solution was observed to be stable upon good storage at both 4 °C and 25 °C for 12 weeks. The DG-THY was observed to remarkably improve in vitro antioxidant activity, in vitro release, and the membrane permeation of THY. The DG-THY ophthalmic solution proved to be very well-tolerated in a rabbit model. The DG-THY ophthalmic solution also demonstrated distinct improvements in the ex vivo and in vivo intraocular permeations of THY. The DG-THY ophthalmic solution also exhibited decreased minimal inhibitory concentrations and minimum bactericidal concentrations of THY. Treatment with the DG-THY ophthalmic solution significantly relieved ocular infection symptoms in rabbit eyes by lowering the number of colony-forming units recovered from the corneas. Therefore, these results demonstrate that DG-THY may be a promising new ophthalmic formulation for the treatment of ocular diseases, especially in terms of oxidative stress-, bacteria-, and inflammation-related eye diseases.
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DG-THY demonstrated remarkable enhancements in in vitro antioxidant activity and membrane permeation properties for THY.
“DG-THY has demonstrated remarkable enhancements regarding both in vitro antioxidant activity and membrane permeation properties for THY.”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [133]
DG-THY ophthalmic solution substantially alleviated inflammatory symptoms and ocular infections in rabbit models through decreasing colony-forming units.
“DG-THY ophthalmic solution substantially alleviated inflammatory symptoms and ocular infections in rabbit models through decreasing colony-forming units [133].”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [133]
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From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics
Sun, M., Wang, J., Fan, W., Wang, K., Wang, Y., Zhang, J., Ding, S., Zhang, C., Feng, Z., Wang, Y.-G., et al. (2025) · Materials today. Bio · doi:10.1016/j.mtbio.2025.102537 · Cited by 7 · see citing works
“DG-THY ophthalmic solution substantially alleviated inflammatory symptoms and ocular infections in rabbit models through decreasing colony-forming units [133].”
- Authors
- Song, K., Yan, M., Li, M., Geng, Y., & Wu, X.
- Affiliations
- Qingdao University of Science and Technology (CN)
- Qingdao Women and Children's Hospital (CN)
- Corresponding author
- Wu, Xianggen
- Venue
- Colloids and Surfaces B Biointerfaces
- Publisher
- Elsevier BV
- Published
- 2020-10
- Volume
- 194
- Pages
- 111157
- ISSN
- 0927-7765 (ISSN-L)
- OpenAlex
- W3030197357
- Cited by
- 35
- References
- 52
- Citations by year
- 2026: 5 · 2025: 8 · 2024: 5 · 2023: 6 · 2022: 6 · 2021: 4 · 2020: 1
- FWCI
- 1.66
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Colloids and Surfaces B Biointerfaces (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Natural Science Foundation of China
- 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
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- thymol, glycyrrhizin, dipotassium glycyrrhizinate, nanomicelles, ocular drug delivery, ophthalmic preparations, topical ocular administration, antioxidant activity, antibacterial activity, ocular infection, rabbit eye model, encapsulation efficiency
- MeSH terms
- Animals, Micelles, Rabbits, Thymol, Drug Delivery Systems, Glycyrrhizic Acid, Administration, Ophthalmic
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