Characterization and evaluation of rapamycin-loaded nano-micelle ophthalmic solution
Open accessAbstract
Rapamycin-loaded nano-micelle ophthalmic solution (RAPA-NM) offers a promising application for preventing corneal allograft rejection; however, RAPA-NM has not yet been fully characterized. This study aimed to evaluate the physicochemical properties, biocompatibility, and underlying mechanism of RAPA-NM in inhibiting corneal allograft rejection. An optimized RAPA-NM was successfully prepared using a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (PVCL-PVA-PEG) graft copolymer as the excipient at a PVCL-PVA-PEG/RAPA weight ratio of 18:1. This formulation exhibited high encapsulation efficiency (99.25 ± 0.55%), small micelle size (64.42 ± 1.18 nm), uniform size distribution (polydispersity index = 0.076 ± 0.016), and a zeta potential of 1.67 ± 0.93 mV. The storage stability test showed that RAPA-NM could be stored steadily for 12 weeks. RAPA-NM also displayed satisfactory cytocompatibility and high membrane permeability. Moreover, topical administration of RAPA-NM could effectively prevent corneal allograft rejection. Mechanistically, a transcriptomic analysis revealed that several immune- and inflammation-related Kyoto Encyclopedia of Genes and Genomes (KEGG) pathways were significantly enriched in the downregulated genes in the RAPA-NM-treated allografts compared with the rejected allogenic corneal grafts. Taken together, these findings highlight the potential of RAPA-NM in treating corneal allograft rejection and other ocular inflammatory diseases.
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RAPA-NM could be stored reliably for 12 weeks while manifesting satisfactory cytocompatibility and high membrane permeability.
“The stability tests indicated that RAPA-NM could be stored reliably for 12 weeks while manifesting satisfactory cytocompatibility and high membrane permeability [152].”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [152]
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- Authors
- Zhang, T., Wei, C., Wu, X., Zhang, S., Duan, F., Qi, X., Shi, W., & Gao, H.
- Affiliations
- Shandong Eye Hospital (CN)
- Shandong First Medical University (CN)
- Qingdao University of Science and Technology (CN)
- Corresponding author
- Shi, Weiyun
- Gao, Hua
- Venue
- Journal of Functional Biomaterials
- Publisher
- MDPI AG
- Published
- 2023-01-16
- Volume
- 14
- Issue
- 1
- Pages
- 49
- ISSN
- 2079-4983 (ISSN-L)
- PMC
- PMC9862165
- OpenAlex
- W4316663537
- Cited by
- 14
- References
- 54
- Citations by year
- 2026: 2 · 2025: 4 · 2024: 5 · 2023: 3
- FWCI
- 1.53
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Journal of Functional Biomaterials (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Funders
- National Nature Science Foundation of China (81870639, 82070923, 2022CXGC010505, 201812150, 202103185, 2019RC009, 2019PT002, 2019ZL001)
- Key R&D Plan of Shandong Province (81870639, 82070923, 2022CXGC010505, 201812150, 202103185, 2019RC009, 2019PT002, 2019ZL001)
- Taishan Scholars Program (81870639, 82070923, 2022CXGC010505, 201812150, 202103185, 2019RC009, 2019PT002, 2019ZL001)
- Academic Promotion Program and Innovation Project of Shandong First Medical University (81870639, 82070923, 2022CXGC010505, 201812150, 202103185, 2019RC009, 2019PT002, 2019ZL001)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Corneal surgery and disorders
- Health Sciences › Medicine › Ophthalmology › Ocular Infections and Treatments
- Keywords
- rapamycin, nanomicelles, eye drops, corneal graft rejection, encapsulation efficiency, cytocompatibility, membrane permeability, topical drug delivery, gene expression profiling, immune pathways, ocular inflammation
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