RT Journal Article
T1 Design, optimization, and in vitro characterization of idebenone-loaded PLGA microspheres for LHON treatment
A1 Varela Fernández, Rubén
A1 Bendicho Lavilla, Carlos
A1 Martín Pastor, Manuel
A1 Herrero-Vanrell, Rocio
A1 Lema Gesto, María Isabel
A1 González Barcia, Luis
A1 Otero Espinar, Francisco Javier
K1 PLGA
K1 Idebenone
K1 LHON
K1 Microparticles
K1 Microspheres
K1 Controlled release
K1 Microencapsulation
K1 Intravitreal administration
AB Biodegradable poly(lactic-co-glycolic acid) microspheres (PLGA MSs) are attractive delivery systems for site-specific maintained release of therapeutic active substances into the intravitreal chamber. The design, development, and characterization of idebenone-loaded PLGA microspheres by means of an oil-in-water emulsion/solvent evaporation method enabled the obtention of appropriate production yield, encapsulation efficiency and loading values. MSs revealed spherical shape, with a size range of 10–25 μm and a smooth and non-porous surface. Fourier-transform infrared spectroscopy (FTIR) spectra demonstrated no chemical interactions between idebenone and polymers. Solid-state nuclear magnetic resonance (NMR), X-ray diffractometry, differential scanning calorimetry (DSC) and thermogravimetry (TGA) analyses indicated that microencapsulation led to drug amorphization. In vitro release profiles were fitted to a biexponential kinetic profile. Idebenone-loaded PLGA MSs showed no cytotoxic effects in an organotypic tissue model. Results suggest that PLGA MSs could be an alternative intraocular system for long-term idebenone administration, showing potential therapeutic advantages as a new therapeutic approach to the Leber's Hereditary Optic Neuropathy (LHON) treatment by intravitreal administration
PB Elsevier
YR 2022
FD 2022
LK http://hdl.handle.net/10347/27623
UL http://hdl.handle.net/10347/27623
LA eng
NO International Journal of Pharmaceutics  616 (2022) 121504
NO This research was partially supported by the Spanish Ministry of Science, Innovation and Universities (RTI2018-099597-B-100)
DS Minerva
RD 29 abr 2026