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Sorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study
Angela Bonaccorso1, Veronica Pepe2, Cristina Zappulla2
1Laboratory of Drug Delivery Technology, Department of Drug and Health Sciences, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
Abstract:
Uveal melanoma is the second most common melanoma and the most common intraocular malignant tumour of the eye. Among various treatments currently studied, Sorafenib was also proposed as a promising drug, often administered with other compounds in order to avoid resistance mechanisms. Despite its promising cellular activities, the use of Sorafenib by oral administration is limited by its severe side effects and the difficulty to reach the target. The encapsulation into drug delivery systems represents an interesting strategy to overcome these limits. In this study, different lipid nanoparticulate formulations were prepared and compared in order to select the most suitable for the encapsulation of Sorafenib. In particular, two solid lipids (Softisan or Suppocire) at different concentrations were used to produce solid lipid nanoparticles, demonstrating that higher amounts were able to achieve smaller particle sizes, higher homogeneity, and longer physical stability. The selected formulations, which demonstrated to be biocompatible on Statens Seruminstitut Rabbit Cornea cells, were modified to improve their mucoadhesion, evaluating the effect of two monovalent cationic lipids with two lipophilic chains. Sorafenib encapsulation allowed obtaining a sustained and prolonged drug release, thus confirming the potential use of the developed strategy to topically administer Sorafenib in the treatment of uveal melanoma.
Insights
Researchers developed novel lipid nanoparticles for topical delivery of Sorafenib, an anti-cancer drug, to treat uveal melanoma. This approach aims to improve drug efficacy and reduce side effects associated with oral administration.
Area of Science:
- Ophthalmology
- Oncology
- Nanotechnology
- Pharmaceutics
Background:
- Uveal melanoma is the most common primary intraocular malignancy.
- Sorafenib shows promise for uveal melanoma treatment but faces challenges with oral administration due to severe side effects and poor target delivery.
- Drug delivery systems offer a strategy to overcome these limitations.
Purpose of the Study:
- To develop and characterize lipid nanoparticulate formulations for topical Sorafenib delivery.
- To enhance mucoadhesion and control drug release for improved ocular treatment.
- To evaluate the potential of these nanoparticles in treating uveal melanoma.
Main Methods:
- Preparation and characterization of solid lipid nanoparticles using Softisan or Suppocire.
- Assessment of particle size, homogeneity, and physical stability.
- Evaluation of biocompatibility on Statens Seruminstitut Rabbit Cornea cells.
- Modification of formulations for mucoadhesion using cationic lipids.
- Encapsulation of Sorafenib and analysis of in vitro drug release profiles.
Main Results:
- Higher concentrations of solid lipids resulted in smaller particle sizes, improved homogeneity, and enhanced physical stability.
- Formulations demonstrated biocompatibility with corneal cells.
- Mucoadhesion was successfully improved.
- Sorafenib encapsulation led to sustained and prolonged drug release.
Conclusions:
- Lipid nanoparticulate formulations are suitable for Sorafenib encapsulation.
- The developed nanoparticles offer a promising strategy for topical delivery of Sorafenib in uveal melanoma treatment.
- This approach may mitigate side effects and improve therapeutic outcomes.
