Design, optimization, and in vitro characterization of idebenone-loaded PLGA microspheres for LHON treatment

[Display omitted] 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 microspher...

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Bibliographic Details
Published in:International journal of pharmaceutics 2022-03, Vol.616, p.121504-121504, Article 121504
Main Authors: Varela-Fernández, Rubén, Bendicho-Lavilla, Carlos, Martin-Pastor, Manuel, Herrero Vanrell, Rocío, Lema-Gesto, María Isabel, González-Barcia, Miguel, Otero-Espinar, Francisco Javier
Format: Article
Language:English
Subjects:
Controlled release
Humans
Idebenone
Intravitreal administration
LHON
Microencapsulation
Microparticles
Microspheres
Optic Atrophy, Hereditary, Leber
Particle Size
PLGA
Polylactic Acid-Polyglycolic Acid Copolymer
Ubiquinone - analogs & derivatives
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Summary:[Display omitted] 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.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2022.121504