Ocular polymeric nanomicelles for the posterior eye segment in the management of retinoblastoma: formulation, optimization, in vitro and ex vivo evaluations
Abstract
The existing study focuses on the development, optimization, and evaluation of sorafenib-loaded polymeric nanomicelles for posterior segment delivery in treating retinoblastoma. The formulation involved adjusting various process and product parameters to create effective drug-loaded polymeric nanomicelles. The particle size, PDI, and zeta potential of optimized formulation were found to be 65.52 ± 1.18 nm, 0.14 ± 0.01, and −3.26 ± 0.66 mV, respectively. The entrapment efficiency and drug release were estimated to be 98.84% ± 0.001 and 99.99% in 6 h, respectively. Additionally, the optimized formulation demonstrated acceptable outcomes for solid-state analysis, osmolality, pH, residual solvent, and morphological properties. After 8 h, the ex vivo transcleral permeation and scleral deposition were 629.05 ± 124.11 ng/cm2 and 4.10 ± 0.54 µg, respectively. Y-79 (human retinoblastoma) cell line study using standard drug, test drug, and optimized formulation revealed anticancer potential at all time points (6, 12, 18, and 24 h) with comparable IC50 values. Furthermore, the optimized formulation exhibited no toxicity on the ARPE-19 (human retinal pigmented epithelium) cell line over 24 h. The optimized formulation was non-irritating to the eye (HET-CAM) and remained stable for 6 months. Thus, drug delivery to the posterior eye segment for the treatment of retinoblastoma appears to be possible with the help of established technology.
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Optimized polymer nanomicelles loaded with sorafenib exhibited excellent transscleral penetration and scleral deposition, showing significant anti-cancer activity against Y-79 cells at all test time points, while being non-toxic to ARPE-19 cells.
“The optimized polymer nanomicelles exhibited excellent transscleral penetration and scleral deposition, showing significant anti-cancer activity against Y-79 cells at all test time points, while being non-toxic to ARPE-19 cells.”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [185]
Sorafenib-loaded polymer nanomicelles are non-irritating to the eyes and remain stable for six months, indicating potential for effective administration to the posterior segment of the eye.
“Furthermore, it is non-irritating to the eyes and remains stable for six months, which indicates that it has the potential to be effectively administered to the posterior segment of the eye [185,186].”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [185]
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From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics
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“Furthermore, it is non-irritating to the eyes and remains stable for six months, which indicates that it has the potential to be effectively administered to the posterior segment of the eye [185,186].”
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- Authors
- Ansari, M., Kulkarni, Y. A., & Singh, K.
- Affiliations
- Narsee Monjee Institute of Management Studies (IN)
- Corresponding author
- Singh, Kavita
- Venue
- Pharmaceutical Development and Technology
- Publisher
- Informa UK Limited
- Published
- 2025-02-23
- Volume
- 30
- Issue
- 3
- Pages
- 246-258
- ISSN
- 1083-7450 (ISSN-L)
- 1097-9867
- OpenAlex
- W4407860016
- Cited by
- 5
- References
- 57
- Citations by year
- 2026: 3 · 2025: 2
- FWCI
- 2.13
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Pharmaceutical Development and Technology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Science and Engineering Research Board (CRG/2020/006376/BHS)
- 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 › Ophthalmology › Ocular Oncology and Treatments
- Keywords
- retinoblastoma, polymeric micelles, sorafenib, ocular drug delivery, ocular toxicity
- MeSH terms
- Sorafenib, Animals, Antineoplastic Agents, Drug Carriers, Humans, Micelles, Particle Size, Polymers, Retinoblastoma, Drug Delivery Systems, Retinal Neoplasms, Cell Line, Tumor, Nanoparticles, Drug Liberation
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