RT Journal Article
T1 Development of an osmoprotective microemulsion as a therapeutic platform for ocular surface protection
A1 López Cano, José Javier
A1 Andrés Guerrero, Vanessa
A1 Vicario De La Torre, Marta
A1 González-Cela Casamayor, Miriam Ana
A1 Benítez Del Castillo Sánchez, José Manuel
A1 Herrero Vanrell, María Del Rocío
A1 Molina Martínez, Irene Teresa
A1 González-Cela Casamayor, Miriam Ana
AB Self-emulsified osmoprotective ophthalmic microemulsions (O/A) were prepared by combining betaine/leucine, clusterin/oleanolic acid, and hyaluronic acid or Dextran. The microemulsions contained an internal oily phase (1.2%), an external aqueous phase (96.3%), cosolvents (1%), and surfactants (1.5%). Physicochemical charac terization and in vivo and in vitro tolerance were analyzed. The formulations’ osmoprotective in vitro activity was assayed in a hyperosmolar model in human corneal cells. Average internal phase sizes were 16–26 nm for the microemulsions including Dextran. Addition of hyaluronic acid increased the size range (25–39 nm). Addition of osmoprotectants did not change nanodroplet size. The formulations were isotonic (280–290 mOsm/L) with neutral pH (≈7) and zeta potential (− 10 to 0 mV), low surface tension (≈35–40 mN⋅m− 1), and low viscosity (≈1 mPa⋅s), except for the microemulsions containing hyaluronic acid (≈4–5 mPa⋅s). SEM and cryo-TEM showed that all formulations exhibited sphere-shaped morphology with good cell tolerance (≈100%) and were stable at 8 ◦C for 9 months. Osmoprotective formulations were well tolerated in vitro and in vivo, protecting cells from hy pertonic stress. We therefore developed stable microemulsions compatible with the ocular surface that could constitute a novel tool for treatment of ophthalmic diseases
PB MDPI
YR 2022
FD 2022-07-25
LK https://hdl.handle.net/20.500.14352/115763
UL https://hdl.handle.net/20.500.14352/115763
LA eng
NO López-Cano JJ, González-Cela-Casamayor MA, Andrés-Guerrero V, Vicario -de-la-Torre M, Benítez Del Castillo JM, Herrero-Vanrell R, et al. Development of an osmoprotective microemulsion as a therapeutic platform for ocular surface protection. International Journal of Pharmaceutics [Internet]. julio de 2022 [citado 23 de enero de 2025];623:121948. Disponible en: https://linkinghub.elsevier.com/retrieve/pii/S0378517322005038
NO Instituto de Salud Carlos III
NO FEDER
NO Universidad Complutense de Madrid
DS Docta Complutense
RD 6 abr 2025