Design of an L-Valine-Modified nanomicelle-based drug delivery system for overcoming ocular surface barriers
Open accessAbstract
The incidence of ocular surface disease (OSD) is increasing, with a trend towards younger ages. However, it is difficult for drugs to reach the deep layers of the cornea due to ocular surface barriers, and bioavailability is less than 5%. In this study, DSPE-PEG2000 was modified with L-valine (L-Val), and an HS15/DSPE-PEG2000-L-Val nanomicelle delivery system containing baicalin (BC) (BC@HS15/DSPE-PEG2000-L-Val) was constructed using thin-film hydration, with a high encapsulation rate, small particle size and no irritation to the ocular surface. Retention experiments on the ocular surface of rabbits and an in vivo corneal permeation test showed that, compared with the control, nanomicelles not only prolonged retention time but also enhanced the ability to deliver drugs to the deep layers of the cornea. The results of a protein inhibition and protein expression assay showed that nanomicelles could increase uptake in human corneal epithelial cells (HCEC) through energy-dependent endocytosis mediated by clathrin, caveolin and the carrier pathway mediated by PepT1 by inhibiting the overexpression of claudin-1 and ZO-1 and suppressing the expression of PepT1-induced by drug stimulation. These results indicate that BC@HS15/DSPE-PEG2000-L-Val is suitable for drug delivery to the deep layers of the ocular surface, providing a potential approach for the development of ocular drug delivery systems.
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BC@HS15/DSPE-PEG2000-L-Val nanomicelles can effectively penetrate the cornea and enhance local drug delivery due to high encapsulation rate, small particle size, and nonirritating effect on the ocular surface.
“In addition, certain locally applied nanocapsules, such as L-valine (L-Val) and an HS15/DSPE-PEG2000-L-Val nanomicelle delivery system containing baicalin (BC) (BC@HS15/DSPE-PEG2000-L-Val), can effectively penetrate the cornea and enhance local drug delivery due to their high encapsulation rate, small particle size and nonirritating effect on the ocular surface.”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [25]
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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
“These findings indicate that nanomicelles not only extend the retention time but also enhance the efficiency to deliver drugs to the deeper layers of cornea [25].”
- Authors
- Wu, H., Xu, Y., Cai, M., You, L., Liu, J., Dong, X., Yin, X., Ni, J., & Qu, C.
- Affiliations
- Beijing University of Chinese Medicine (CN)
- Corresponding author
- Ni, Jian
- Qu, Changhai
- ORCID
- Venue
- Pharmaceutics
- Publisher
- MDPI AG
- Published
- 2022-06-16
- Volume
- 14
- Issue
- 6
- Pages
- 1277
- ISSN
- 1999-4923 (ISSN-L)
- PMC
- PMC9230556
- OpenAlex
- W4283071414
- Cited by
- 18
- References
- 48
- Citations by year
- 2026: 4 · 2025: 7 · 2024: 2 · 2023: 4 · 2022: 1
- FWCI
- 1.45
- Type
- journal article
- Language
- en
- Update notices
- correction (2022-06-16)
- Open access
- gold
- doi.org
- Licence
- Locations
- Pharmaceutics (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Funders
- Beijing Natural Science Foundation (7202123)
- 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 › Public Health, Environmental and Occupational Health › Ocular Surface and Contact Lens
- Keywords
- ocular drug delivery, ocular surface barrier, baicalin, corneal permeation, corneal epithelial cells, clathrin-mediated endocytosis, caveolin, claudin-1, ZO-1, PepT1, PEGylated liposomes, ocular surface disease
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