Hyaluronan-Cholesterol Nanogels for the Enhancement of the Ocular Delivery of Therapeutics

The anatomy and physiology of the eye strongly limit the bioavailability of locally administered drugs. The entrapment of therapeutics into nanocarriers represents an effective strategy for the topical treatment of several ocular disorders, as they may protect the embedded molecules, enabling drug r...

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Autores principales:	Nicole Zoratto, Laura Forcina, Roberto Matassa, Luciana Mosca, Giuseppe Familiari, Antonio Musarò, Maurizio Mattei, Tommasina Coviello, Chiara Di Meo, Pietro Matricardi
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	hyaluronan nanogels ocular delivery permeation enhancer Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/9b4c0d59d5114554a5031705a204466d
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spelling	oai:doaj.org-article:9b4c0d59d5114554a5031705a204466d2021-11-25T18:40:38ZHyaluronan-Cholesterol Nanogels for the Enhancement of the Ocular Delivery of Therapeutics10.3390/pharmaceutics131117811999-4923https://doaj.org/article/9b4c0d59d5114554a5031705a204466d2021-10-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1781https://doaj.org/toc/1999-4923The anatomy and physiology of the eye strongly limit the bioavailability of locally administered drugs. The entrapment of therapeutics into nanocarriers represents an effective strategy for the topical treatment of several ocular disorders, as they may protect the embedded molecules, enabling drug residence on the ocular surface and/or its penetration into different ocular compartments. The present work shows the activity of hyaluronan-cholesterol nanogels (NHs) as ocular permeation enhancers. Thanks to their bioadhesive properties, NHs firmly interact with the superficial corneal epithelium, without penetrating the stroma, thus modifying the transcorneal penetration of loaded therapeutics. <i>Ex vivo</i> transcorneal permeation experiments show that the permeation of hydrophilic drugs (i.e., tobramycin and diclofenac sodium salt), loaded in NHs, is significantly enhanced when compared to the free drug solutions. On the other side, the permeation of hydrophobic drugs (i.e., dexamethasone and piroxicam) is strongly dependent on the water solubility of the entrapped molecules. The obtained results suggest that NHs formulations can improve the ocular bioavailability of the instilled drugs by increasing their preocular retention time (hydrophobic drugs) or facilitating their permeation (hydrophilic drugs), thus opening the route for the application of HA-based NHs in the treatment of both anterior and posterior eye segment diseases.Nicole ZorattoLaura ForcinaRoberto MatassaLuciana MoscaGiuseppe FamiliariAntonio MusaròMaurizio MatteiTommasina CovielloChiara Di MeoPietro MatricardiMDPI AGarticlehyaluronannanogelsocular deliverypermeation enhancerPharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1781, p 1781 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	hyaluronan nanogels ocular delivery permeation enhancer Pharmacy and materia medica RS1-441
spellingShingle	hyaluronan nanogels ocular delivery permeation enhancer Pharmacy and materia medica RS1-441 Nicole Zoratto Laura Forcina Roberto Matassa Luciana Mosca Giuseppe Familiari Antonio Musarò Maurizio Mattei Tommasina Coviello Chiara Di Meo Pietro Matricardi Hyaluronan-Cholesterol Nanogels for the Enhancement of the Ocular Delivery of Therapeutics
description	The anatomy and physiology of the eye strongly limit the bioavailability of locally administered drugs. The entrapment of therapeutics into nanocarriers represents an effective strategy for the topical treatment of several ocular disorders, as they may protect the embedded molecules, enabling drug residence on the ocular surface and/or its penetration into different ocular compartments. The present work shows the activity of hyaluronan-cholesterol nanogels (NHs) as ocular permeation enhancers. Thanks to their bioadhesive properties, NHs firmly interact with the superficial corneal epithelium, without penetrating the stroma, thus modifying the transcorneal penetration of loaded therapeutics. <i>Ex vivo</i> transcorneal permeation experiments show that the permeation of hydrophilic drugs (i.e., tobramycin and diclofenac sodium salt), loaded in NHs, is significantly enhanced when compared to the free drug solutions. On the other side, the permeation of hydrophobic drugs (i.e., dexamethasone and piroxicam) is strongly dependent on the water solubility of the entrapped molecules. The obtained results suggest that NHs formulations can improve the ocular bioavailability of the instilled drugs by increasing their preocular retention time (hydrophobic drugs) or facilitating their permeation (hydrophilic drugs), thus opening the route for the application of HA-based NHs in the treatment of both anterior and posterior eye segment diseases.
format	article
author	Nicole Zoratto Laura Forcina Roberto Matassa Luciana Mosca Giuseppe Familiari Antonio Musarò Maurizio Mattei Tommasina Coviello Chiara Di Meo Pietro Matricardi
author_facet	Nicole Zoratto Laura Forcina Roberto Matassa Luciana Mosca Giuseppe Familiari Antonio Musarò Maurizio Mattei Tommasina Coviello Chiara Di Meo Pietro Matricardi
author_sort	Nicole Zoratto
title	Hyaluronan-Cholesterol Nanogels for the Enhancement of the Ocular Delivery of Therapeutics
title_short	Hyaluronan-Cholesterol Nanogels for the Enhancement of the Ocular Delivery of Therapeutics
title_full	Hyaluronan-Cholesterol Nanogels for the Enhancement of the Ocular Delivery of Therapeutics
title_fullStr	Hyaluronan-Cholesterol Nanogels for the Enhancement of the Ocular Delivery of Therapeutics
title_full_unstemmed	Hyaluronan-Cholesterol Nanogels for the Enhancement of the Ocular Delivery of Therapeutics
title_sort	hyaluronan-cholesterol nanogels for the enhancement of the ocular delivery of therapeutics
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/9b4c0d59d5114554a5031705a204466d
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Hyaluronan-Cholesterol Nanogels for the Enhancement of the Ocular Delivery of Therapeutics

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