García Otero, XurxoVarela Fernández, RubénCuartero Martínez, AndreaGómez Lado, NoemíGonzález Barcia, MiguelMondelo García, CristinaFeitosa, CarolinaAguiar Fernández, PabloFernández Ferreiro, AnxoOtero Espinar, Francisco Javier2025-06-302025-06-302025-01-27García-Otero, X., Varela-Fernández, R., Cuartero-Martínez, A., Gómez-Lado, N., González-Barcia, M., Mondelo-García, C., Feitosa, C., Aguiar, P., Fernández-Ferreiro, A. and Otero-Espinar, F.J. (2025), Intravitreal Administration of Adalimumab-Loaded Poly(Lactic-co-Glycolic Acid) Nanoparticles: Effects on Biodistribution and Pharmacokinetics. Small Sci., 5: 2400494. https://doi.org/10.1002/smsc.202400494https://hdl.handle.net/10347/42354Adalimumab, a monoclonal antibody used for treating inflammatory diseases, including eye diseases, faces challenges in biodistribution and targeted delivery. Nanoparticle (NP)-based drug delivery systems have shown promise in enhancing the pharmacokinetic profiles of biologic drugs. This study aims to develop, and characterize intravitreal adalimumab-loaded poly(lactic-co-glycolic acid) (PLGA) NPs to improve antibody distribution and therapeutic efficacy. Characterization studies, morphological examination, and quantitative, stability, and physical properties are conducted. In vitro release kinetics are assessed using a dialysis membrane method. In vivo biodistribution is studied in rats after intravitreal administration by Positron Emission Tomography/Computed Tomography imaging. The optimized NPs were spherical (around 300 nm) with a surface charge of about −20 mV. Encapsulation efficiency and drug loading reach values close to 100%. Stability studies showed minimal changes in particle size and drug content. In vitro release showed a biphasic pattern with an initial burst release followed by sustained release. Safety studies indicated no significant cytotoxicity or adverse effects. The adalimumab-loaded PLGA NPs demonstrate favorable physicochemical characteristics, stability, and release profiles. In vivo distribution revealed a change in the antibody's distribution pattern after intravitreal administration via NPs encapsulation. These findings suggest the potential for enhanced therapeutic outcomes and warrant further investigation in disease-specific models to explore the clinical potential of this NP-based delivery system.eng© 2024 The Author(s). Small Science published by Wiley-VCH GmbH.This is an open access article under the terms of the CreativeCommons Attribution License, which permits use, distribution andreproduction in any medium, provided the original work is properly cited.Attribution 4.0 Internationalhttp://creativecommons.org/licenses/by/4.0/AdalimumabControlled releasesIn vivo distribution and pharmacokineticsNanoparticlesPoly(lactic-co-glycolic acid)Intravitreal Administration of Adalimumab-Loaded Poly(Lactic-co-Glycolic Acid) Nanoparticles: Effects on Biodistribution and Pharmacokineticsjournal article10.1002/smsc.2024004942688-4046open access