Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-A
The physiological protective mechanisms of the eye reduce the bioavailability of topically administered drugs above all for those with high molecular weight and /or lipophilic characteristics, such as Cyclosporine A (CyA). The combined strategy based on the association of nanomicelles and mucoadhesi...
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doaj-1ccd38b3ffd34676b81c1aa0af49ce202020-11-25T02:01:59ZengMDPI AGPharmaceutics1999-49232020-03-0112325310.3390/pharmaceutics12030253pharmaceutics12030253Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-AEleonora Terreni0Patrizia Chetoni1Silvia Tampucci2Susi Burgalassi3Ali Athab Al-kinani4Raid G. Alany5Daniela Monti6Department of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyDrug Discovery, Delivery and Patient Care (DDDPC) Theme, School of Life Sciences, Pharmacy and Chemistry, Kingston University London, Kingston upon Thames, London KT1 2EE, UKDrug Discovery, Delivery and Patient Care (DDDPC) Theme, School of Life Sciences, Pharmacy and Chemistry, Kingston University London, Kingston upon Thames, London KT1 2EE, UKDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyThe physiological protective mechanisms of the eye reduce the bioavailability of topically administered drugs above all for those with high molecular weight and /or lipophilic characteristics, such as Cyclosporine A (CyA). The combined strategy based on the association of nanomicelles and mucoadhesive polymer seems promising since a limited number of commercial products containing CyA have been recently approved. The scope of this investigation was the design of Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano), based on a binary system of two surfactants in combination with hyaluronic acid, and their biopharmaceutical evaluation. The optimisation of the ASMP-Nano in term of the amount of surfactants, CyA-loading and size determined the selection of the clear and stable Nano1HAB-CyA formulation containing 0.105% <i>w</i>/<i>w</i> CyA loaded-nanomicelles with a size of 14.41 nm. The nanostructured system had a protective effect towards epithelial corneal cells with a cell viability of more than 80%. It interacted with cellular barriers favouring the uptake and the accumulation of CyA into the cells as evidenced by fluorescent probe distribution, by hindering CyA permeation through reconstituted corneal epithelial tissue. In pharmacokinetics study on rabbits, the nanomicellar carrier prolonged the CyA retention time in the precorneal area mainly in presence of hyaluronic acid (HA), a mucoadhesive polymer.https://www.mdpi.com/1999-4923/12/3/253nanomicellesocular pharmacokineticrabbitshyaluronic acidvitamin e-tpgscyclosporine areconstituted corneal tissue |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Eleonora Terreni Patrizia Chetoni Silvia Tampucci Susi Burgalassi Ali Athab Al-kinani Raid G. Alany Daniela Monti |
spellingShingle |
Eleonora Terreni Patrizia Chetoni Silvia Tampucci Susi Burgalassi Ali Athab Al-kinani Raid G. Alany Daniela Monti Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-A Pharmaceutics nanomicelles ocular pharmacokinetic rabbits hyaluronic acid vitamin e-tpgs cyclosporine a reconstituted corneal tissue |
author_facet |
Eleonora Terreni Patrizia Chetoni Silvia Tampucci Susi Burgalassi Ali Athab Al-kinani Raid G. Alany Daniela Monti |
author_sort |
Eleonora Terreni |
title |
Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-A |
title_short |
Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-A |
title_full |
Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-A |
title_fullStr |
Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-A |
title_full_unstemmed |
Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-A |
title_sort |
assembling surfactants-mucoadhesive polymer nanomicelles (asmp-nano) for ocular delivery of cyclosporine-a |
publisher |
MDPI AG |
series |
Pharmaceutics |
issn |
1999-4923 |
publishDate |
2020-03-01 |
description |
The physiological protective mechanisms of the eye reduce the bioavailability of topically administered drugs above all for those with high molecular weight and /or lipophilic characteristics, such as Cyclosporine A (CyA). The combined strategy based on the association of nanomicelles and mucoadhesive polymer seems promising since a limited number of commercial products containing CyA have been recently approved. The scope of this investigation was the design of Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano), based on a binary system of two surfactants in combination with hyaluronic acid, and their biopharmaceutical evaluation. The optimisation of the ASMP-Nano in term of the amount of surfactants, CyA-loading and size determined the selection of the clear and stable Nano1HAB-CyA formulation containing 0.105% <i>w</i>/<i>w</i> CyA loaded-nanomicelles with a size of 14.41 nm. The nanostructured system had a protective effect towards epithelial corneal cells with a cell viability of more than 80%. It interacted with cellular barriers favouring the uptake and the accumulation of CyA into the cells as evidenced by fluorescent probe distribution, by hindering CyA permeation through reconstituted corneal epithelial tissue. In pharmacokinetics study on rabbits, the nanomicellar carrier prolonged the CyA retention time in the precorneal area mainly in presence of hyaluronic acid (HA), a mucoadhesive polymer. |
topic |
nanomicelles ocular pharmacokinetic rabbits hyaluronic acid vitamin e-tpgs cyclosporine a reconstituted corneal tissue |
url |
https://www.mdpi.com/1999-4923/12/3/253 |
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