Self-assembling topical nanomicellar formulation to improve curcumin absorption across ocular tissues
Abstract
The pathophysiological mechanisms for dry and wet age-related macular degeneration (AMD) involve oxidative stress and increased VEGF release and expression. An ideal drug candidate for both types of AMD is the one which offers significant protection to the retinal cells from oxidative stress and inhibit VEGF release. Curcumin is one such natural product which provides numerous beneficial effects including antioxidant, anti-inflammatory, and anti-VEGF activities and has the potential for the treatment of both types of AMD. The bioavailability of curcumin is negligible due to its poor aqueous solubility. The purpose of this work is to develop an aqueous nanomicellar drop formulation of curcumin (CUR-NMF) for back of the eye delivery utilizing hydrogenated castor oil (HCO-40) and octoxynol-40 (OC-40) to treat AMD. A full factorial design was performed with JMP software analysis to optimize the formulation size, polydispersity index (PDI), entrapment efficiency, loading, and precipitation. MTT and LDH assays on human retinal pigmented epithelial (D407) cells revealed that 5-10 μM CUR-NMF dose is safe for ophthalmic use. Furthermore, CUR-NMF exhibited significant protection of retinal (D407) cells against H 2 O 2-induced oxidative stress. In vitro drug release kinetics suggested a sustained drug release profile indicating a long-term protection ability of CUR-NMF against oxidative stress to retinal cells. In addition, an ELISA suggested that CUR-NMF significantly reduces vascular endothelial growth factor (VEGF) release in D407 cell line, hence diminishes the risk of angiogenesis. Collectively, these results suggest that the proposed CUR-NMF can be tremendously effective in treating both types of AMD.
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CUR-NMF significantly reduced VEGF release in D407 cell lines, thus diminishing the risk of angiogenesis.
“In addition, ELISA results indicated that CUR-NMF significantly reduced VEGF release in D407 cell lines, thus diminishing the risk of angiogenesis [196].”
From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [196]
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“In addition, ELISA results indicated that CUR-NMF significantly reduced VEGF release in D407 cell lines, thus diminishing the risk of angiogenesis [196].”
- Authors
- Alshamrani, M., Sikder, S., Coulibaly, F., Mandal, A., Pal, D., & Mitra, A. K.
- Affiliations
- University of Missouri–Kansas City (US)
- Corresponding author
- Mitra, Ashim K.
- Venue
- AAPS PharmSciTech
- Published
- 2019-07-17
- Volume
- 20
- Issue
- 7
- Pages
- 254-254
- ISSN
- 1530-9932 (ISSN-L)
- OpenAlex
- W2957038649
- Cited by
- 46
- References
- 35
- Citations by year
- 2026: 7 · 2025: 4 · 2024: 6 · 2023: 7 · 2022: 7 · 2021: 7 · 2020: 8
- FWCI
- 2.35
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- AAPS PharmSciTech (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Medicine › Curcumin's Biomedical Applications
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- curcumin, age-related macular degeneration, ocular drug delivery, hydrogenated castor oil, self-assembly, retinal pigment epithelial cells, oxidative stress, VEGF inhibition, sustained drug release, bioavailability
- MeSH terms
- Antioxidants, Biological Availability, Castor Oil, Cell Line, Curcumin, Delayed-Action Preparations, Eye, Humans, Micelles, Oxidative Stress, Vascular Endothelial Growth Factor A, Nanostructures, Administration, Ophthalmic
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