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...
| Authors: | ; ; ; ; ; |
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| Format: | Article |
| Publication date: | 2011 |
| Country: | España |
| Institution: | Universidad Complutense de Madrid (UCM) |
| Repository: | Docta Complutense |
| Language: | English |
| OAI Identifier: | oai:docta.ucm.es:20.500.14352/45149 |
| Online Access: | https://hdl.handle.net/20.500.14352/45149 |
| Access Level: | Open access |
| Keyword: | 617.7 615.357 54-126 Melatonin Polymer Eye Química orgánica (Química) Oftalmología Oftalmología veterinaria 2306 Química Orgánica 3201.09 Oftalmología |
| _version_ | 1878729112699273216 |
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| author | Andrés Guerrero, Vanesa |
| 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 |
| author_browse | Andrés Guerrero, Vanesa Heras Polo, Beatriz De Las Herrero Vanrell, María Del Rocío Molina Martínez, Irene Teresa Peral Cerda, María Asunción Pintor Just, Jesús Jerónimo |
| 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 |
| collection | Docta Complutense |
| 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. |
| eu_rights_str_mv | openAccess |
| format | article |
| id | ES_01acb256ea762d3df140cb1e77b4c6df |
| institution | Universidad Complutense de Madrid (UCM) |
| instname_str | Universidad Complutense de Madrid (UCM) |
| language | eng |
| network_acronym_str | ES |
| network_name_str | España |
| oai_identifier_str | oai:docta.ucm.es:20.500.14352/45149 |
| publishDate | 2011 |
| publishDateSort | 2011 |
| publisher | Association for Research in Vision and Ophthalmology (ARVO) |
| publisherStr | Association for Research in Vision and Ophthalmology (ARVO) |
| reponame_str | Docta Complutense |
| spelling | The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit Eyes 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 617.7 615.357 54-126 Melatonin Polymer Eye Química orgánica (Química) Oftalmología Oftalmología veterinaria 2306 Química Orgánica 3201.09 Oftalmología 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. Association for Research in Vision and Ophthalmology (ARVO) https://hdl.handle.net/20.500.14352/45149 |
| 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 | 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_short | 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 |
| topic | 617.7 615.357 54-126 Melatonin Polymer Eye Química orgánica (Química) Oftalmología Oftalmología veterinaria 2306 Química Orgánica 3201.09 Oftalmología |
| topic_facet | 617.7 615.357 54-126 Melatonin Polymer Eye Química orgánica (Química) Oftalmología Oftalmología veterinaria 2306 Química Orgánica 3201.09 Oftalmología |
| url | https://hdl.handle.net/20.500.14352/45149 |