Topical application of polymeric nanomicelles in ophthalmology: a review on research efforts for the noninvasive delivery of ocular therapeutics
Abstract
INTRODUCTION: Polymeric micelles represent nowadays an interesting formulative approach for ocular drug delivery, as they act as solubility enhancers of poorly soluble drugs and promote drug transport across cornea and sclera. In particular, in the last 5 years polymeric nanomicelles have been increasingly investigated to overcome some of the important challenges of the topical treatment of ocular diseases. AREAS COVERED: The aim of this review was to gather up-to-date information on the different roles that polymeric micelles (commonly in the nanosize scale) can play in ocular delivery. Thus, after a general description of ocular barriers and micelles features, the attention is focused on those properties that are relevant for ophthalmic application. Finally, their efficacy in improving the ocular delivery of different classes of therapeutics (anti-inflammatory, immunosuppressant, antiglaucoma, antifungal, and antiviral drugs) are reported. EXPERT OPINION: Although still a few, in vivo experiments have clearly demonstrated the capability of polymeric nanomicelles to overcome a variety of hurdles associated to ocular therapy, notably increasing drug bioavailability. However, there are still some very important issues to be solved, such as tolerability and stability; additionally, the role of micelles in drug uptake by the ocular tissues and their potential for the treatment of posterior eye diseases still need to be clarified/verified.
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Growing evidence indicates that nanomicelles can be utilized for addressing ocular surface inflammation, retinal degeneration and vascular proliferative disorders.
“Growing evidence indicates that nanomicelles can be utilized for addressing ocular surface inflammation, retinal degeneration and vascular proliferative disorders [93].”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [93]
The most investigated administration route for micelles is intravenous injection/infusion, mainly for chemotherapy, but improved drug bioavailability has also been reported following oral and topical administration.
“The most investigated administration route for micelles is the intravenous (i.v.) injection/infusion (mainly exploited for chemotherapy) [18,[47][48][49], but very interesting results in terms of improved drug bioavailability have also been reported following oral [31,50] and topical (ocular, nasal, buccal) [26,36,51,52] administration.”
From Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions (2021) · cites this paper as [51]
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Pescina, S., Santi, P., Ferrari, G., & Nicoli, S. (2011) · Therapeutic Delivery · doi:10.4155/tde.11.104 · Cited by 20 · see citing works
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Clear, Aqueous Topical Drop of Triamcinolone Acetonide
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Ghezzi, M., Pescina, S., Padula, C., Santi, P., Del Favero, E., Cantù, L., & Nicoli, S. (2021) · Journal of Controlled Release · doi:10.1016/j.jconrel.2021.02.031 · Cited by 1,135 · see citing works
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Self-citationMicelle-nanogel platform for ferulic acid ocular delivery
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Joy, R., George, J., & John, F. (2022) · ChemistrySelect · doi:10.1002/slct.202104045 · Cited by 50 · see citing works
Self-assembling tacrolimus nanomicelles for retinal drug delivery
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Self-citationAlambiaga-Caravaca, A. M., Calatayud-Pascual, M. A., Rodilla, V., Concheiro, A., López-Castellano, A., & Alvarez-Lorenzo, C. (2020) · Pharmaceutics · doi:10.3390/pharmaceutics12080702 · Cited by 38 · see citing works
From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics
Sun, M., Wang, J., Fan, W., Wang, K., Wang, Y., Zhang, J., Ding, S., Zhang, C., Feng, Z., Wang, Y.-G., et al. (2025) · Materials today. Bio · doi:10.1016/j.mtbio.2025.102537 · Cited by 7 · see citing works
“Growing evidence indicates that nanomicelles can be utilized for addressing ocular surface inflammation, retinal degeneration and vascular proliferative disorders [93].”
- Authors
- Grimaudo, M. A., Pescina, S., Padula, C., Santi, P., Concheiro, A., Alvarez-Lorenzo, C., & Nicoli, S.
- Affiliations
- University of Parma (IT)
- Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, R+DPharma Group (GI-1645), Facultad de Farmacia and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, Santiago de Compostela, Spain
- Corresponding author
- Nicoli, Sara
- ORCID
- Venue
- Expert Opinion on Drug Delivery
- Publisher
- Informa UK Limited
- Published
- 2019-04-03
- Volume
- 16
- Issue
- 4
- Pages
- 397-413
- ISSN
- 1742-5247 (ISSN-L)
- 1744-7593
- OpenAlex
- W2923651815
- Cited by
- 78
- References
- 111
- Citations by year
- 2026: 4 · 2025: 8 · 2024: 11 · 2023: 13 · 2022: 16 · 2021: 10 · 2020: 12 · 2019: 4
- FWCI
- 1.00
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Expert Opinion on Drug Delivery (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- polymeric micelles, ocular drug delivery, topical ophthalmic therapy, poorly water-soluble drugs, ocular barriers, drug bioavailability, glaucoma medications, antifungal agents, antiviral agents, anti-inflammatory agents, immunosuppressants
- MeSH terms
- Animals, Biological Availability, Cornea, Drug Compounding, Eye Diseases, Humans, Micelles, Polymers, Sclera, Solubility, Drug Delivery Systems, Administration, Ophthalmic
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