Sorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study

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 pro...

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Autores principales:	Angela Bonaccorso, Veronica Pepe, Cristina Zappulla, Cinzia Cimino, Angelo Pricoco, Giovanni Puglisi, Francesco Giuliano, Rosario Pignatello, Claudia Carbone
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	nanomedicine drug repurposing Softisan 100 uveal melanoma mucoadhesion eye irritation test Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/e94956e7b86747de9d67b8015e8c67b5
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spelling	oai:doaj.org-article:e94956e7b86747de9d67b8015e8c67b52021-11-25T18:42:21ZSorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study10.3390/pharmaceutics131119561999-4923https://doaj.org/article/e94956e7b86747de9d67b8015e8c67b52021-11-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1956https://doaj.org/toc/1999-4923Uveal 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.Angela BonaccorsoVeronica PepeCristina ZappullaCinzia CiminoAngelo PricocoGiovanni PuglisiFrancesco GiulianoRosario PignatelloClaudia CarboneMDPI AGarticlenanomedicinedrug repurposingSoftisan 100uveal melanomamucoadhesioneye irritation testPharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1956, p 1956 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	nanomedicine drug repurposing Softisan 100 uveal melanoma mucoadhesion eye irritation test Pharmacy and materia medica RS1-441
spellingShingle	nanomedicine drug repurposing Softisan 100 uveal melanoma mucoadhesion eye irritation test Pharmacy and materia medica RS1-441 Angela Bonaccorso Veronica Pepe Cristina Zappulla Cinzia Cimino Angelo Pricoco Giovanni Puglisi Francesco Giuliano Rosario Pignatello Claudia Carbone Sorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study
description	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.
format	article
author	Angela Bonaccorso Veronica Pepe Cristina Zappulla Cinzia Cimino Angelo Pricoco Giovanni Puglisi Francesco Giuliano Rosario Pignatello Claudia Carbone
author_facet	Angela Bonaccorso Veronica Pepe Cristina Zappulla Cinzia Cimino Angelo Pricoco Giovanni Puglisi Francesco Giuliano Rosario Pignatello Claudia Carbone
author_sort	Angela Bonaccorso
title	Sorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study
title_short	Sorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study
title_full	Sorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study
title_fullStr	Sorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study
title_full_unstemmed	Sorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study
title_sort	sorafenib repurposing for ophthalmic delivery by lipid nanoparticles: a preliminary study
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/e94956e7b86747de9d67b8015e8c67b5
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Sorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study

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