PLA–PCL–PEG–PCL–PLA based micelles for improving the ocular permeability of dexamethasone: development, characterization, and in vitro evaluation
Abstract
The aim of the present research was to investigate the feasibility of developing polylactide–polycaprolactone–polyethylene glycol–polycaprolactone–polylactide (PLA–PCL–PEG–PCL–PLA) based micelles to improve ocular permeability of dexamethasone (DEX). PLA–PCL–PEG–PCL–PLA copolymers were synthesized by a ring-opening polymerization method. DEX was loaded into the developed copolymers. The DEX-loaded micelles were characterized using transmission electron microscopy (TEM) and dynamic light scattering (DLS) methods. Cytotoxicity of the micelles obtained was investigated on L929 cell line. Cellular uptake was followed by fluorescence microscopy and flow cytometry analyses. The release behavior of DEX from the micelles as well as the drug release kinetics was studied. Corneal permeability was also evaluated using an ex vivo bovine model. The pentablock copolymers were successfully synthesized. The TEM results verified the formation of spherical micelles, the sizes of which was approximately 65 nm. The micelles exhibited suitable compatibility on L929 cells. The release profile showed an initial burst release phase followed by a sustained release phase, the kinetic of which was close to the Weibull’s distribution model. The micelles showed higher corneal permeability in comparison to a marketed DEX eye drop. Taken together, the results indicated that the PLA–PCL–PEG–PCL–PLA micelles could be appropriate candidates for the ocular delivery of DEX, and probably other hydrophobic drugs.
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PLA-PCL-PEG-PCL-PLA micelles had suitable compatibility with L929 cells and were internalized by these cells in a concentration- and time-dependent manner.
“The micelles had suitable compatibility with L929 cells and were internalized by these cells in a concentration- and time-dependent manner.”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [174]
PCL-PEG-PCL and PLA-PCL-PEG-PCL-PLA micelles could serve as promising candidates for ocular delivery of DEX as well as potentially other steroid drugs.
“Taken together, these findings suggest that PCL-PEG-PCL and PLA-PCL-PEG-PCL-PLA micelles could serve as promising candidates for ocular delivery of DEX as well as potentially other steroid drugs [174].”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [174]
At 24 h and 36 h post-injection, PLA-PCL-PEG-PCL-PLA micelles exhibited superior inhibitory effects on uveitis compared with marketed eye drops.
“At 24 h and 36 h post-injection, PLA-PCL-PEG-PCL-PLA micelles exhibited superior inhibitory effects on uveitis compared with marketed eye drops.”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [174]
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“Taken together, these findings suggest that PCL-PEG-PCL and PLA-PCL-PEG-PCL-PLA micelles could serve as promising candidates for ocular delivery of DEX as well as potentially other steroid drugs [174].”
- Authors
- Alami-Milani, M., Zakeri-Milani, P., Valizadeh, H., Fathi, M., Salatin, S., Salehi, R., & Jelvehgari, M.
- Affiliations
- Tabriz University of Medical Sciences (IR)
- Liver and Gastrointestinal Diseases Research Center, Tabriz University of Medical Sciences, Tabriz, Iran;
- Corresponding author
- Jelvehgari, Mitra
- Venue
- Pharmaceutical Development and Technology
- Publisher
- Informa UK Limited
- Published
- 2020-03-08
- Volume
- 25
- Issue
- 6
- Pages
- 704-719
- ISSN
- 1083-7450 (ISSN-L)
- 1097-9867
- OpenAlex
- W3008045423
- Cited by
- 36
- References
- 89
- Citations by year
- 2026: 1 · 2025: 5 · 2024: 4 · 2023: 13 · 2022: 5 · 2021: 7 · 2012: 1
- FWCI
- 2.44
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Pharmaceutical Development and Technology (publishedVersion)
- PubMed (publishedVersion)
- 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
- dexamethasone, ocular drug delivery, micelles, pentablock copolymers, corneal permeability, sustained drug release, ring-opening polymerization, hydrophobic drug delivery, ocular toxicity, Weibull release kinetics
- MeSH terms
- Drug Development, Animals, Anti-Inflammatory Agents, Cattle, Cell Line, Cornea, Dexamethasone, Drug Evaluation, Preclinical, Micelles, Organ Culture Techniques, Permeability, Polyesters, Polyethylene Glycols, Mice
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