Imatinib-loaded micelles of hyaluronic acid derivatives for potential treatment of neovascular ocular diseases
Abstract
In this work, new micellar systems able to cross corneal barrier and to improve the permeation of imatinib free base were prepared and characterized. HA-EDA-C 16, HA-EDA-C 16 –PEG, and HA-EDA-C 16 –CRN micelles were synthesized starting from hyaluronic acid (HA), ethylenediamine (EDA), hexadecyl chains (C 16 ), polyethylene glycol (PEG), or l -carnitine (CRN). These nanocarriers showed optimal particle size and mucoadhesive properties. Imatinib-loaded micelles were able to interact with corneal barrier and to promote imatinib transcorneal permeation and penetration. In addition, a study was conducted to understand the in vitro imatinib inhibitory effect on a choroidal neovascularization process. Imatinib released from polymeric micelles was able to inhibit endothelial cell sprouting and to promote cell tube disruption.
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Compared with administration of free drug, imatinib significantly inhibited endothelial cell tube formation while promoting disruption of cell tubes within the EHS matrix.
“Compared with the administration of free drug, imatinib significantly inhibited endothelial cell tube formation while promoting disruption of cell tubes within the EHS matrix.”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [167]
Imatinib-loaded micelles were capable of interacting with the corneal barrier, thereby promoting transcorneal permeation of imatinib.
“Above all, these micelles were capable of interacting with the corneal barrier, thereby promoting transcorneal permeation of imatinib [167].”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [167]
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Yongvongsoontorn, N., Chung, J. E., & Kurisawa, M. (2026) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2026.108088
Bai, Y., Liu, L., Li, C., Ma, Y., Liu, P., & Wang, S. (2026) · Molecules · doi:10.3390/molecules31071169
- Authors
- Bongiovì, F., Fiorica, C., Palumbo, F. S., Di Prima, G., Giammona, G., & Pitarresi, G.
- Affiliations
- University of Palermo (IT)
- Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy
- National Research Council (IT)
- Corresponding author
- Pitarresi, Giovanna
- Venue
- Molecular Pharmaceutics
- Publisher
- American Chemical Society (ACS)
- Published
- 2018-09-24
- Volume
- 15
- Issue
- 11
- Pages
- 5031-5045
- ISSN
- 1543-8384 (ISSN-L)
- 1543-8392
- OpenAlex
- W2892518235
- Cited by
- 44
- References
- 49
- Citations by year
- 2026: 1 · 2025: 8 · 2024: 6 · 2023: 5 · 2022: 5 · 2021: 8 · 2020: 7 · 2019: 4
- FWCI
- 2.23
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Molecular Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Nova Science Publishers (Nova Science Publishers, Inc.) (submittedVersion)
- Funders
- Ministero dell?Istruzione, dell?Universit? e della Ricerca (PON01_01434)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Keywords
- imatinib, polymeric micelles, hyaluronic acid derivatives, ethylenediamine, corneal permeation, choroidal neovascularization, mucoadhesion, drug release, PEG, L-carnitine
- MeSH terms
- Imatinib Mesylate, Animals, Carnitine, Cattle, Cell Line, Cell Survival, Cornea, Drug Carriers, Drug Compounding, Ethylenediamines, Humans, Hyaluronic Acid, Micelles, Particle Size, Permeability, Polyethylene Glycols, Choroidal Neovascularization, Endothelial Cells, Protein Kinase Inhibitors, Administration, Ophthalmic, Drug Liberation
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