Self-assembling tacrolimus nanomicelles for retinal drug delivery
Open accessAbstract
Neovascular age-related macular degeneration (AMD) is characterized by an increase in reactive oxygen species (ROS) and pro-inflammatory cytokines in the retinal pigment epithelium cells. The primary purpose of this study was the development of a clear, tacrolimus nanomicellar formulation (TAC-NMF) for AMD. The optimized formulation had a mean diameter of 15.41 nm, a zeta potential of 0.5 mV, and an entrapment efficiency of 97.13%. In-vitro cytotoxicity studies revealed the dose-dependent cytotoxicity of TAC-NMF on various ocular cell lines, such as human retinal pigment epithelium (D407), monkey retinal choroidal endothelial (RF/6A) cells, and human corneal epithelium (CCL 20.2) cells. Cellular uptake and in-vitro distribution studies using flow cytometry and confocal microscopy, respectively, indicated an elevated uptake of TAC-NMF in a time-dependent manner. Biocompatibility assay using macrophage RAW 264.7 cell line resulted in low production of inflammatory cytokines such as IL-6, IL-1β and TNF-α after treatment with TAC-NMF. There was a decrease in ROS in D407 cells pre-treated with sodium iodate (ROS inducing agent) after treating with TAC-NMF and tacrolimus drug. Similarly, there was a reduction in the pro-inflammatory cytokines and VEGF-A in D407 cells pretreated with sodium iodate. This indicates that TAC-NMF could lower pro-inflammatory cytokines and ROS commonly seen in AMD.
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TAC-NMF can effectively diminish pro-inflammatory cytokines and ROS commonly seen in AMD.
“These findings indicate that TAC-NMF can effectively diminish pro-inflammatory cytokines and ROS commonly seen in AMD [194].”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [194]
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From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics
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- Authors
- Gote, V., Mandal, A., Alshamrani, M., & Pal, D.
- Affiliations
- University of Missouri–Kansas City (US)
- Corresponding author
- Pal, Dhananjay
- Venue
- Pharmaceutics
- Publisher
- MDPI AG
- Published
- 2020-11-10
- Volume
- 12
- Issue
- 11
- Pages
- 1072
- ISSN
- 1999-4923 (ISSN-L)
- PMC
- PMC7698121
- OpenAlex
- W3102464703
- Cited by
- 39
- References
- 58
- Citations by year
- 2026: 5 · 2025: 7 · 2024: 10 · 2023: 7 · 2022: 3 · 2021: 7
- FWCI
- 1.65
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Pharmaceutics (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Health Sciences › Medicine › Ophthalmology › Retinal Diseases and Treatments
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- tacrolimus, nanomicelles, self-assembly, neovascular age-related macular degeneration, retinal drug delivery, retinal pigment epithelium, reactive oxygen species, inflammatory cytokines, VEGF-A, cytotoxicity, cellular uptake, biocompatibility, anti-inflammatory nanomedicine
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