Functionalization of polymeric nanomicelles and mixed nanomicelles for targeted retinal delivery in the management of retinoblastoma
Abstract
The current research discusses polymer conjugation, formulation development, and evaluation of sorafenib-loaded polymeric nanomicelles of conjugated soluplus (solu-tin) and polymeric mixed nanomicelles of conjugated soluplus (solu-tin) with conjugated poloxamer 188 (polo-tin) for site-specific posterior segment delivery to the retina in managing retinoblastoma. Firstly, the soluplus and poloxamer 188 were conjugated with biotin by Fischer esterification reaction and evaluated by FTIR and 1 H NMR for confirmation of covalent bond formation involving the carboxyl group of biotin and hydroxyl group of polymers. Secondly, the sorafenib-loaded solu-tin nanomicelles and mixed nanomicelles of solu-tin with polo-tin were formulated by the thin film hydration method. Thereafter, these nanomicelles were evaluated and displayed suitable outcomes for particle size (78.53 nm and 73.17 nm), PDI (0.089 and 0.074), zeta potential (-3.65 mV and -4.17 mv), entrapment efficiency (99.23 % and 99.83 %), in vitro drug release (4 h and 8 h), solid-state analysis, osmolality (290 mOsm/kg and 293 mOsm/kg), pH (7.4 and 7.4), TEM (spherical) and residual solvent analysis (287.90 ppm and 363.49 ppm). The ex vivo transcleral permeation at 8 h was found to be 548.45 ng/cm 2 and 281.61 ng/cm 2, respectively. Both the drug-loaded nanomicelles displayed a dose-dependent anticancer effect on Y-79 cells at all time points i.e. 6, 12, 18, and 24 h, and were non-toxic to normal retinal pigmented epithelial cell line (ARPE-19) when incubated for 24 h. Furthermore, the formulations were non-irritant (HET-CAM) and stable for 6 months. Hence, the developed technology is safe and efficacious for targeting the retina in managing retinoblastoma.
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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 [186]
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 [186]
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- Authors
- Ansari, M., Gupta, C., Kulkarni, Y. A., & Singh, K.
- Affiliations
- Narsee Monjee Institute of Management Studies (IN)
- Bombay College of Pharmacy (IN)
- Corresponding author
- Singh, Kavita
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2025-02
- Volume
- 671
- Pages
- 125235
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W4406504881
- Cited by
- 10
- References
- 68
- Citations by year
- 2026: 2 · 2025: 8
- FWCI
- 4.23
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Department of Science and Technology, Ministry of Science and Technology, India (CRG/2020/006376/BHS)
- Science and Engineering Research Board
- 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 › Drug Solubulity and Delivery Systems
- Keywords
- retinoblastoma, polymeric micelles, sorafenib, Soluplus, poloxamer 188, biotin conjugation, Fischer esterification, Y79 cells, ocular drug delivery
- MeSH terms
- Sorafenib, Animals, Antineoplastic Agents, Biotin, Cell Survival, Drug Carriers, Humans, Micelles, Particle Size, Polyethylene Glycols, Polymers, Polyvinyls, Retina, Retinoblastoma, Drug Delivery Systems, Retinal Neoplasms, Poloxamer, Cell Line, Tumor, Nanoparticles, Drug Liberation
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