Cited by 18Advanced Drug Delivery SystemsNanoparticle-Based Drug DeliveryOcular Surface and Contact Lens

Design of an L-Valine-Modified nanomicelle-based drug delivery system for overcoming ocular surface barriers

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Wu, Huimin, Xu, Yuchen, Cai, Mengru, You, Longtai, Liu, Jing, Dong, Xiaoxv, Yin, Xingbin, Ni, Jian +1 more·2022·Pharmaceutics

Abstract

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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Crossref · 10.3390/pharmaceutics14061277

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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.”

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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
Venue
Pharmaceutics
Publisher
MDPI AG
Published
2022-06-16
Volume
14
Issue
6
Pages
1277
ISSN
1999-4923 (ISSN-L)
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
Open access
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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