Hybrid formulations of liposomes and bioadhesive polymers improve the hypotensive effect of the melatonin analogue 5-mca-nat in rabbit eyes.

DANIELA QUINTEROS; MARTA VICARIO-DE-LA-TORRE; VANESSA ANDRÉS-GUERRERO; SANTIAGO PALMA; DANIEL ALLEMANDI; ROCIO HERRERO-VANRELL; IRENE MOLINA-MARTÍNEZ

PUBLIC LIBRARY SCIENCE

Lugar: San Francisco; Año: 2014 vol. 9

or the treatment of chronic ocular diseases such as glaucoma, continuous instillations of eye drops are needed. However, frequent administrations of hypotensive topical formulations can produce adverse ocular surface effects due to the active substance or other components of the formulation, such as preservatives or other excipients. Thus the development of unpreserved formulations that are well tolerated after frequent instillations is an important challenge to improve ophthalmic chronic topical therapies. Furthermore, several components can improve the properties of the formulation in terms of efficacy. In order to achieve the mentioned objectives, we have developed formulations of liposomes (150?200 nm) containing components similar to those in the tear film and loaded with the hypotensive melatonin analog 5- methoxycarbonylamino-N-acetyltryptamine (5-MCA-NAT, 100 mM). These formulations were combined with mucoadhesive(sodium hyaluronate or carboxymethylcellulose) or amphiphilic