2026-06-27T12:32:05Zhttps://docta.ucm.es/rest/oai/request
oai:docta.ucm.es:20.500.14352/70732024-07-31T14:29:23Zcom_20.500.14352_14col_20.500.14352_15
Docta Complutense author Villa Hermosilla, M. C. author Fernández Carballido, Ana María author Fernández-Carballido, Ana author Hurtado, Carolina author Barcia Hernández, Emilia María author Montejo, Consuelo author Alonso, Mario author Negro Álvarez, María Sofía Elisa 2023-06-17T08:25:36Z 2023-06-17T08:25:36Z 2021-06-24 1999-4923 10.3390/pharmaceutics13070951 https://hdl.handle.net/20.500.14352/7073 https://doi.org/10.3390/pharmaceutics13070951 http://www.mdpi.com/journal/pharmaceutics Rheumatoid arthritis (RA) is a chronic inflammatory disease with sulfasalazine (SSZ) extensively used for long-term treatment of both juvenile and adult RA. Its use is associated with adverse effects and toxicity due to its non-selective biodistribution. Macrophages play an important role in inflammatory processes. In order to target SSZ to macrophages in this work two microparticulate systems (MPs) are developed: SSZ-loaded PLGA MPs without and with α-tocopherol, with particle sizes lower than 5 μm and encapsulation efficiencies of 81.07 ± 11% and 63.50 ± 6.62%, respectively. Release of SSZ from MPs prepared with α-tocopherol was prolonged for 20 days. In RAW 264.7 cell macrophages MPs prepared with α-tocopherol were captured faster. Cell viability studies confirmed that SSZ-loaded MPs prepared without and with α-tocopherol did not produce cytotoxicity at the concentrations assayed. The anti-inflammatory activity of SSZ-loaded MPs was studied by quantifying interleukins IL-1, IL-6 and TNF-α in macrophages. All formulations produced a significant reduction of cytokine concentrations after 24 and 72 h, indicating that release of SSZ from the MPs was able to inhibit the inflammatory response induced by lipopolysaccharide (LPS). Gene expression of IL-1, IL-6 and TNF-α was decreased by SSZ-loaded MPs. SSZ-loaded MPs prepared with α-tocopherol will potentially allow increasing the residence time of SSZ in the synovial cavity, prolonging its duration of action, and reducing the adverse effects associated with its non-selective biodistribution. eng Atribución 3.0 España Sulfasalazine Microparticles Targeting Macrophages for the Treatment of Inflammatory Diseases Affecting the Synovial Cavity journal article URL https://docta.ucm.es/bitstreams/570131ac-1846-4c29-b193-7d5c81fca8cf/download File MD5 a0121e3c29b0478cac746013446b272b 4242788 application/pdf pharmaceutics-13-00951-v2.pdf