RT Journal Article
T1 Enhancing the hypotensive effect of latanoprost by combining synthetic phosphatidylcholine liposomes with hyaluronic acid and osmoprotective agents
A1 Brugnera, Marco
A1 Vicario De La Torre, Marta
A1 González-Cela Casamayor, Miriam Ana
A1 López Cano, José Javier
A1 Bravo Osuna, Irene
A1 Huete Toral, Fernando
A1 González Rubio, María Luisa
A1 Carracedo Rodríguez, Juan Gonzalo
A1 Molina Martínez, Irene Teresa
A1 Andrés Guerrero, Vanesa
A1 Herrero Vanrell, María Del Rocío
AB The first line of glaucoma treatment focuses on reducing intraocular pressure (IOP) through the prescription of topical prostaglandin analogues, such as latanoprost (LAT). Topical ophthalmic medicines have low bioavailability due to their rapid elimination from the ocular surface. Nanotechnology offers innovative ways of enhancing the ocular bioavailability of antiglaucoma agents while reducing administration frequency. This study aims to combine LAT-loaded synthetic phosphatidylcholine liposomes with hyaluronic acid (0.2% w/v) and the osmoprotectants betaine (0.40% w/v) and leucine (0.90% w/v) (LAT-HA-LIP) to extend the hypotensive effect of LAT while protecting the ocular surface. LAT-HA-LIP was prepared as a mixture of 1,2-dioleoyl-sn-glycero-3-phosphocholine and 1,2-dimyristoyl-sn-glycero-3-phosphocholine, cholesterol and α-tocopherol acetate. LAT-HA-LIP exhibited high drug-loading capacity (104.52 ± 4.10%), unimodal vesicle sizes (195.14 ± 14.34 nm) and a zeta potential of -13.96 ± 0.78 mV. LAT-HA-LIP was isotonic (284.00 ± 1.41 mOsm L-1), had neutral pH (7.63 ± 0.01) and had suitable surface tension (44.07 ± 2.70 mN m-1) and viscosity (2.69 ± 0.15 mPa s-1) for topical ophthalmic administration. LAT-HA-LIP exhibited optimal in vitro tolerance in human corneal and conjunctival epithelial cells. No signs of ocular alteration or discomfort were observed when LAT-HA-LIP was instilled in albino male New Zealand rabbits. Hypotensive studies revealed that, after a single eye drop, the effect of LAT-HA-LIP lasted 24 h longer than that of a marketed formulation and that relative ocular bioavailability was almost three times higher (p < 0.001). These findings indicate the potential ocular protection and hypotensive effect LAT-HA-LIP offers in glaucoma treatment.
PB Springer
YR 2024
FD 2024-04-11
LK https://hdl.handle.net/20.500.14352/104840
UL https://hdl.handle.net/20.500.14352/104840
LA eng
NO Brugnera M, Vicario-de-la-Torre M, González-Cela Casamayor MA, López-Cano JJ, Bravo-Osuna I, Huete-Toral F, González Rubio ML, Carracedo G, Molina-Martínez IT, Andrés-Guerrero V, Herrero-Vanrell R. Enhancing the hypotensive effect of latanoprost by combining synthetic phosphatidylcholine liposomes with hyaluronic acid and osmoprotective agents. Drug Deliv Transl Res. 2024 Apr 11. doi: 10.1007/s13346-024-01584-z. Epub ahead of print. PMID: 38602615.
NO Universidad Complutense de Madrid
NO European Research Council
DS Docta Complutense
RD 12 abr 2025