RT Journal Article
T1 Comparison of the in vitro tolerance and in vivo efficacy of traditional timolol maleate eye drops versus new formulations with bioadhesive polymers
A1 Andrés Guerrero, Vanesa
A1 Vicario De La Torre, Marta
A1 Molina Martínez, Irene Teresa
A1 Benítez Del Castillo Sánchez, José Manuel
A1 García Feijoo, Julián
A1 Herrero Vanrell, María Del Rocío
AB PURPOSE. To assess the in vitro tolerance and in vivo efficacy of new unpreserved formulations of timolol maleate (TM) in aqueous solutions of bioadhesive polymers used for dry eye treatment and to compare them with three traditional TM formulations: unpreserved Timabak (Thea, Madrid, Spain), benzalkonium chloride (BAK)-preserved Timoftol (Frosst Laboratories, Madrid, Spain), and BAK-preserved Timolol Sandoz (Frosst Laboratories). METHODS. New formulations were composed of TM (0.5%) and carboxymethyl cellulose (0.5%), hyaluronic acid (0.2%), or hydroxypropylmethyl cellulose (0.3% or 0.5%). In vitro tolerance was determined in human corneal-limbal epithelial cells and normal human conjunctival cells. The ocular hypotensive effect was evaluated measuring IOP in rabbit eyes for 8 hours. RESULTS. In all cases, cell survival after exposure to the formulations was greater in the new unpreserved TM formulations than in the traditional TM solutions (BAK-preserved and unpreserved). In addition, the new formulations were demonstrated to maintain the hypotensive effect of TM in different magnitudes. The maximum hypotensive effect was reached by TM 0.5% in carboxymethyl cellulose 0.5% (32.37%).CONCLUSIONS. The results demonstrated that new unpreserved formulations of TM with bioadhesive polymers decreased IOP in rabbits and reached values closer to those reached by traditional solutions. Furthermore, new formulations presented a significantly higher in vitro tolerance than the same compound in traditional formulations. Although unpreserved formulations are usually more expensive, preservative-free antiglaucoma eye drops should improve compliance and adherence in the medical treatment of glaucoma. Bioadhesive polymers could be part of antiglaucoma formulations to reduce ocular toxicity, improve drug efficacy, and protect the ocular surface in long-term therapies.
SN 1552-5783
YR 2011
FD 2011-06
LK https://hdl.handle.net/20.500.14352/97724
UL https://hdl.handle.net/20.500.14352/97724
LA eng
NO Ministerio de Sanidad(España)
NO Fondo de Investigaciones Sanitarias
NO Universidad Complutense de Madrid
DS Docta Complutense
RD 9 abr 2025