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.
Highlights
Among the intraocular malignant tumours affecting the inner eye, the most common in adults is uveal melanoma (UM) [1]
As reported in the literature, nanoparticle size strongly affects drug distribution and residence time in the eye’s structure, with nanoparticles smaller than 200 nm usually showing a burst release followed by a gradual release profile in vitro and a longer half-life, compared to smaller nanoparticles characterised by a longer half-life and a sustained drug release [21,22]
In order to obtain homogeneous small-sized solid lipid nanoparticles (SLN) for potential ophthalmic application, a preliminary quali-quantitative screening was developed on two different solid lipids, Softisan (A) and Suppocire (B), at different concentrations (5, 7, 8, 9 % w/v)
Summary
Among the intraocular malignant tumours affecting the inner eye, the most common in adults is uveal melanoma (UM) [1]. The pigmentation could have a protective function since a risk factor is having a lightly coloured iris [3]. Characteristic of this melanoma is the great ability to metastasise 34%), and the most affected organ is the liver (90%), with lungs and soft tissues following [4].
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
