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Protective Role and Enhanced Intracellular Uptake of Curcumin in Retinal Cells Using Self-Emulsifying Drug Delivery
Elide Zingale1,2,3, Sebastiano Masuzzo1, Tatu Lajunen4,5
1Department of Drug and Health Sciences, University of Catania, 95125 Catania, Italy.
Pharmaceuticals (Basel, Switzerland)
|February 26, 2025
Summary
This study developed self-nanoemulsifying drug delivery systems (SNEDDS) for curcumin (CUR) to treat diabetic retinopathy (DR). The novel CUR-SNEDDS formulation enhances ocular delivery, antioxidant activity, and Sirtuin-1 (SIRT1) expression in retinal cells.
Area of Science:
- Ocular pharmacology and drug delivery
- Biomedical engineering
- Molecular biology
Background:
- Sirtuin-1 (SIRT1) is crucial for protecting ocular tissues from degenerative diseases.
- Reduced SIRT1 levels are linked to diabetic retinopathy (DR), necessitating SIRT1-boosting therapies.
- Curcumin (CUR) is a potential SIRT1 agonist, but its poor solubility and ocular penetration limit topical delivery.
Purpose of the Study:
- To develop and characterize self-nanoemulsifying drug delivery systems (SNEDDS) for topical ocular delivery of curcumin (CUR).
- To evaluate the efficacy of CUR-SNEDDS in enhancing CUR delivery, antioxidant activity, and SIRT1 expression in retinal cells.
Main Methods:
- Optimized CUR-loaded SNEDDS were prepared and characterized for physicochemical and technological properties after reconstitution with simulated tear fluid.
- In vitro assessments included entrapment efficiency, stability, drug release, mucoadhesion, cytotoxicity on human corneal epithelial (HCE) cells, antioxidant activity in retinal pigment epithelial (ARPE-19) cells, and cellular uptake.
- SIRT1 expression levels were measured following treatment with CUR-SNEDDS.
Main Results:
- CUR-SNEDDS exhibited high entrapment efficiency (~99%) and stability in simulated tear fluid.
- Modified CUR-SNEDDS showed enhanced mucoadhesion and superior antioxidant activity compared to free CUR.
- CUR-SNEDDS demonstrated good cytocompatibility, increased cellular uptake in retinal cells, and effectively induced SIRT1 expression.
Conclusions:
- The developed CUR-SNEDDS are a promising formulation for topical ocular delivery of curcumin.
- These systems offer improved retinal delivery, antioxidant effects, and potential therapeutic benefits for DR.
- The enhanced cellular uptake and SIRT1 induction highlight the potential of SNEDDS for treating ocular diseases.
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