The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit Eyes

Purpose.: 5-Methoxy-carbonylamino-N-acetyltryptamine (5-MCA-NAT, a melatonin receptor agonist) produces a clear intraocular pressure (IOP) reduction in New Zealand White rabbits and glaucomatous monkeys. The goal of this study was to evaluate whether the hypotensive effect of 5-MCA-NAT was enhanced...

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Autores: Andrés Guerrero, Vanesa, Molina Martínez, Irene Teresa, Peral Cerda, María Asunción, Heras Polo, Beatriz De Las, Pintor Just, Jesús Jerónimo, Herrero Vanrell, María Del Rocío
Tipo de recurso: artículo
Fecha de publicación:2011
País:España
Institución:Universidad Complutense de Madrid (UCM)
Repositorio:Docta Complutense
Idioma:inglés
OAI Identifier:oai:docta.ucm.es:20.500.14352/45149
Acceso en línea:https://hdl.handle.net/20.500.14352/45149
Access Level:acceso abierto
Palabra clave:617.7
615.357
54-126
Melatonin
Polymer
Eye
Química orgánica (Química)
Oftalmología
Oftalmología veterinaria
2306 Química Orgánica
3201.09 Oftalmología
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oai_identifier_str oai:docta.ucm.es:20.500.14352/45149
network_acronym_str ES
network_name_str España
repository_id_str
spelling The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit EyesAndrés Guerrero, VanesaMolina Martínez, Irene TeresaPeral Cerda, María AsunciónHeras Polo, Beatriz De LasPintor Just, Jesús JerónimoHerrero Vanrell, María Del Rocío617.7615.35754-126MelatoninPolymerEyeQuímica orgánica (Química)OftalmologíaOftalmología veterinaria2306 Química Orgánica3201.09 OftalmologíaPurpose.: 5-Methoxy-carbonylamino-N-acetyltryptamine (5-MCA-NAT, a melatonin receptor agonist) produces a clear intraocular pressure (IOP) reduction in New Zealand White rabbits and glaucomatous monkeys. The goal of this study was to evaluate whether the hypotensive effect of 5-MCA-NAT was enhanced by the presence of cellulose derivatives, some of them with bioadhesive properties, as well as to determine whether these formulations were well tolerated by the ocular surface. Methods.: Formulations were prepared with propylene glycol (0.275%), carboxymethyl cellulose (CMC, 0.5% and 1.0%) of low and medium viscosity and hydroxypropylmethyl cellulose (0.3%). Quantification of 5-MCA-NAT (100 μM) was assessed by HPLC. In vitro tolerance was evaluated by the MTT method in human corneal-limbal epithelial cells and normal human conjunctival cells. In vivo tolerance was analyzed by biomicroscopy and specular microscopy in rabbit eyes. The ocular hypotensive effect was evaluated measuring IOP for 8 hours in rabbit eyes. Results.: All the formulations demonstrated good in vitro and in vivo tolerance. 5-MCA-NAT in CMC medium viscosity 0.5% was the most effective at reducing IOP (maximum IOP reduction, 30.27%), and its effect lasted approximately 7 hours. Conclusions.: The hypotensive effect of 5-MCA-NAT was increased by using bioadhesive polymers in formulations that are suitable for the ocular surface and also protective of the eye in long-term therapies. The use of 5-MCA-NAT combined with bioadhesive polymers is a good strategy in the treatment of ocular hypertension and glaucoma.Association for Research in Vision and Ophthalmology (ARVO)Universidad Complutense de Madrid20112011-03-0120112011-03-01journal articlehttp://purl.org/coar/resource_type/c_6501info:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/20.500.14352/45149reponame:Docta Complutenseinstname:Universidad Complutense de Madrid (UCM)Inglésengopen accesshttp://purl.org/coar/access_right/c_abf2Atribución-NoComercial-SinDerivadas 3.0 Españahttps://creativecommons.org/licenses/by-nc-nd/3.0/es/info:eu-repo/semantics/openAccessoai:docta.ucm.es:20.500.14352/451492026-06-02T12:44:21Z
dc.title.none.fl_str_mv The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit Eyes
title The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit Eyes
spellingShingle The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit Eyes
Andrés Guerrero, Vanesa
617.7
615.357
54-126
Melatonin
Polymer
Eye
Química orgánica (Química)
Oftalmología
Oftalmología veterinaria
2306 Química Orgánica
3201.09 Oftalmología
title_short The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit Eyes
title_full The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit Eyes
title_fullStr The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit Eyes
title_full_unstemmed The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit Eyes
title_sort The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit Eyes
dc.creator.none.fl_str_mv Andrés Guerrero, Vanesa
Molina Martínez, Irene Teresa
Peral Cerda, María Asunción
Heras Polo, Beatriz De Las
Pintor Just, Jesús Jerónimo
Herrero Vanrell, María Del Rocío
author Andrés Guerrero, Vanesa
author_facet Andrés Guerrero, Vanesa
Molina Martínez, Irene Teresa
Peral Cerda, María Asunción
Heras Polo, Beatriz De Las
Pintor Just, Jesús Jerónimo
Herrero Vanrell, María Del Rocío
author_role author
author2 Molina Martínez, Irene Teresa
Peral Cerda, María Asunción
Heras Polo, Beatriz De Las
Pintor Just, Jesús Jerónimo
Herrero Vanrell, María Del Rocío
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv Universidad Complutense de Madrid
dc.subject.none.fl_str_mv 617.7
615.357
54-126
Melatonin
Polymer
Eye
Química orgánica (Química)
Oftalmología
Oftalmología veterinaria
2306 Química Orgánica
3201.09 Oftalmología
topic 617.7
615.357
54-126
Melatonin
Polymer
Eye
Química orgánica (Química)
Oftalmología
Oftalmología veterinaria
2306 Química Orgánica
3201.09 Oftalmología
description Purpose.: 5-Methoxy-carbonylamino-N-acetyltryptamine (5-MCA-NAT, a melatonin receptor agonist) produces a clear intraocular pressure (IOP) reduction in New Zealand White rabbits and glaucomatous monkeys. The goal of this study was to evaluate whether the hypotensive effect of 5-MCA-NAT was enhanced by the presence of cellulose derivatives, some of them with bioadhesive properties, as well as to determine whether these formulations were well tolerated by the ocular surface. Methods.: Formulations were prepared with propylene glycol (0.275%), carboxymethyl cellulose (CMC, 0.5% and 1.0%) of low and medium viscosity and hydroxypropylmethyl cellulose (0.3%). Quantification of 5-MCA-NAT (100 μM) was assessed by HPLC. In vitro tolerance was evaluated by the MTT method in human corneal-limbal epithelial cells and normal human conjunctival cells. In vivo tolerance was analyzed by biomicroscopy and specular microscopy in rabbit eyes. The ocular hypotensive effect was evaluated measuring IOP for 8 hours in rabbit eyes. Results.: All the formulations demonstrated good in vitro and in vivo tolerance. 5-MCA-NAT in CMC medium viscosity 0.5% was the most effective at reducing IOP (maximum IOP reduction, 30.27%), and its effect lasted approximately 7 hours. Conclusions.: The hypotensive effect of 5-MCA-NAT was increased by using bioadhesive polymers in formulations that are suitable for the ocular surface and also protective of the eye in long-term therapies. The use of 5-MCA-NAT combined with bioadhesive polymers is a good strategy in the treatment of ocular hypertension and glaucoma.
publishDate 2011
dc.date.none.fl_str_mv 2011
2011-03-01
2011
2011-03-01
dc.type.none.fl_str_mv journal article
http://purl.org/coar/resource_type/c_6501
dc.type.openaire.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv https://hdl.handle.net/20.500.14352/45149
url https://hdl.handle.net/20.500.14352/45149
dc.language.none.fl_str_mv Inglés
eng
language_invalid_str_mv Inglés
language eng
dc.rights.none.fl_str_mv open access
http://purl.org/coar/access_right/c_abf2
Atribución-NoComercial-SinDerivadas 3.0 España
https://creativecommons.org/licenses/by-nc-nd/3.0/es/
dc.rights.openaire.fl_str_mv info:eu-repo/semantics/openAccess
rights_invalid_str_mv open access
http://purl.org/coar/access_right/c_abf2
Atribución-NoComercial-SinDerivadas 3.0 España
https://creativecommons.org/licenses/by-nc-nd/3.0/es/
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Association for Research in Vision and Ophthalmology (ARVO)
publisher.none.fl_str_mv Association for Research in Vision and Ophthalmology (ARVO)
dc.source.none.fl_str_mv reponame:Docta Complutense
instname:Universidad Complutense de Madrid (UCM)
instname_str Universidad Complutense de Madrid (UCM)
reponame_str Docta Complutense
collection Docta Complutense
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,300719

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