RT Journal Article
T1 The Use of Mucoadhesive Polymers to Enhance the Hypotensive Effect of a Melatonin Analogue, 5-MCA-NAT, in Rabbit Eyes
A1 Andrés Guerrero, Vanesa
A1 Molina Martínez, Irene Teresa
A1 Peral Cerda, María Asunción
A1 Heras Polo, Beatriz De Las
A1 Pintor Just, Jesús Jerónimo
A1 Herrero Vanrell, María Del Rocío
AB 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.
PB Association for Research in Vision and Ophthalmology (ARVO)
SN 1552-5783
YR 2011
FD 2011-03
LK https://hdl.handle.net/20.500.14352/45149
UL https://hdl.handle.net/20.500.14352/45149
LA eng
NO Revista en O.A. en la web del editor
NO Ministerio de Sanidad (España)
NO Ministerio de Ciencia, Innovación y Universidades (España)
NO Grupo de Investigación de la Universidad Complutense UCM-920415
NO Grupo de Investigación de la Universidad Complutense UCM-920777
NO Universidad Complutense de Madrid
DS Docta Complutense
RD 9 abr 2025