Cited by 87Advanced Drug Delivery SystemsNanoparticle-Based Drug DeliveryAdvancements in Transdermal Drug Delivery

Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration

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Li, Jingguo, Li, Zhanrong, Zhou, Tianyang, Zhang, Junjie, Xia, Huiyun, Li, Heng, He, Jijun, He, Siyu +1 more·2015·International Journal of Nanomedicine

Abstract

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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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
Published
2015-09
Volume
10
Pages
6027
ISSN
  • 1176-9114 (ISSN-L)
  • 1178-2013
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
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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