Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration
Open accessAbstract
PURPOSE: The cornea is a main barrier to drug penetration after topical application. The aim of this study was to evaluate the abilities of micelles generated from a positively charged triblock copolymer to penetrate the cornea after topical application. METHODS: The triblock copolymer poly(ethylene glycol)-poly(ε-caprolactone)-g-polyethyleneimine was synthesized, and the physicochemical properties of the self-assembled polymeric micelles were investigated, including hydrodynamic size, zeta potential, morphology, drug-loading content, drug-loading efficiency, and in vitro drug release. Using fluorescein diacetate as a model drug, the penetration capabilities of the polymeric micelles were monitored in vivo using a two-photon scanning fluorescence microscopy on murine corneas after topical application. RESULTS: The polymer was successfully synthesized and confirmed using nuclear magnetic resonance and Fourier transform infrared. The polymeric micelles had an average particle size of 28 nm, a zeta potential of approximately +12 mV, and a spherical morphology. The drug-loading efficiency and drug-loading content were 75.37% and 3.47%, respectively, which indicates that the polymeric micelles possess a high drug-loading capacity. The polymeric micelles also exhibited controlled-release behavior in vitro. Compared to the control, the positively charged polymeric micelles significantly penetrated through the cornea. CONCLUSION: Positively charged micelles generated from a triblock copolymer are a promising vehicle for the topical delivery of hydrophobic agents in ocular applications.
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Self-citation
- Authors
- Li, J., Li, Z., Zhou, T., Zhang, J., Xia, H., Li, H., He, J., He, S., & Wang, L.
- Affiliations
- Zhengzhou University (CN)
- Corresponding author
- Zhang, Junjie
- Venue
- International Journal of Nanomedicine
- Publisher
- Informa UK Limited
- Published
- 2015-09
- Volume
- 10
- Pages
- 6027
- ISSN
- 1176-9114 (ISSN-L)
- 1178-2013
- PMC
- PMC4592048
- OpenAlex
- W1811964762
- Cited by
- 87
- References
- 39
- Citations by year
- 2026: 2 · 2025: 11 · 2024: 12 · 2023: 13 · 2022: 5 · 2021: 12 · 2020: 10 · 2019: 4 · 2018: 10 · 2017: 5 · 2016: 3
- FWCI
- 3.32
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- International Journal of Nanomedicine (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)
- Dove Medical Press (Taylor and Francis Group) (submittedVersion, cc-by-nc)
- Funders
- Zhengzhou Municipal Science and Technology Bureau
- National Natural Science Foundation of China (21504082, 81170831, 81270991, U1304811, U1404832)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Keywords
- triblock copolymers, corneal penetration, topical ocular drug delivery, fluorescein diacetate, two-photon fluorescence microscopy, controlled drug release, hydrophobic drug delivery, corneal barrier
- MeSH terms
- Animals, Cornea, Mice, Inbred C57BL, Micelles, Particle Size, Polyesters, Polyethylene Glycols, Polymers, Microscopy, Confocal, Mice, Hydrophobic and Hydrophilic Interactions
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