RT Journal Article
T1 Infliximab microencapsulation: an innovative approach for intra-articular administration of biologics in the management of rheumatoid arthritis-in vitro evaluation
A1 Lamela Gómez, Iván
A1 Gonçalves, Lídia M.
A1 Almeida, António J.
A1 Luzardo Álvarez, Asteria María
K1 Infliximab
K1 Microencapsulation
K1 Rheumatoid arthritis
K1 Intra-articular
K1 Controlled release
K1 Monoclonal antibodies
AB Microencapsulation of the therapeutical monoclonal antibody infliximab (INF) was investigated as an innovative approach to improve its stability and to achieve formulations with convenient features for intra-articular administration. Ultrasonic atomization (UA), a novel alternative to microencapsulate labile drugs, was compared with the conventional emulsion/evaporation method (Em/Ev) using biodegradable polymers, specifically Polyactive® 1000PEOT70PBT30 [poly(ethylene-oxide-terephthalate)/poly(butylene-terephthalate); PEOT-PBT] and its polymeric blends with poly-(D, L-lactide-co-glycolide) (PLGA) RG502 and RG503 (PEOT-PBT:PLGA; 65:35). Six different formulations of spherical core-shell microcapsules were successfully developed and characterized. The UA method achieved a significantly higher encapsulation efficiency (69.7-80.25%) than Em/Ev (17.3-23.0%). Mean particle size, strongly determined by the microencapsulation method and to a lesser extent by polymeric composition, ranged from 26.6 to 49.9 µm for UA and 1.5-2.1 µm for Em/Ev. All formulations demonstrated sustained INF release in vitro for up to 24 days, with release rates modulated by polymeric composition and microencapsulation technique. Both methods preserved INF biological activity, with microencapsulated INF showing higher efficacy than commercial formulations at comparable doses regarding bioactive tumor necrosis factor-alpha (TNF-α) neutralization according to WEHI-13VAR bioassay. Microparticles' biocompatibility and extensive internalization by THP-1-derived macrophages was demonstrated. Furthermore, high in vitro anti-inflammatory activity was achieved after treatment of THP-1 cells with INF-loaded microcapsules, significatively reducing in vitro production of TNF-α and interleucine-6 (Il-6)
PB Springer
SN 2190-393X
YR 2023
FD 2023
LK http://hdl.handle.net/10347/30851
UL http://hdl.handle.net/10347/30851
LA eng
NO Lamela-Gómez I, Gonçalves LM, Almeida AJ, Luzardo-Álvarez A. Infliximab microencapsulation: an innovative approach for intra-articular administration of biologics in the management of rheumatoid arthritis-in vitro evaluation. Drug Deliv Transl Res. 2023 Jun 9. doi: 10.1007/s13346-023-01372-1. Epub ahead of print. PMID: 37294425.
NO Open Access funding provided thanks to the CRUE-CSIC agreement with Springer Nature. Iván Lamela-Gómez received funding from the “Axudas á etapa predoutoral da Xunta de Galicia, cofinanciadas polo programa operativo FSE Galicia 2014–2020” predoctoral grant program. Consellería de Cultura, Educación e ordenación universitaria, Xunta de Galicia, Spain. This research was partially funded by Consellería de Cultura, Educación e ordenación universitaria, Xunta de Galicia, Spain. Axudas para a consolidación e estructuración deunidades de investigación competitivas Modalidad A: Grupos de Referencia Competitiva (ED341C 2017/13). This research was also partially funded by the Fundação para a Ciência e a Tecnologia (FCT), Portugal (UID/DTP/04138/2019 and UIDB/04138/2020 to iMed.ULisboa), and principal investigator grants CEECIND/03143/2017 (L. M. Gonçalves)
DS Minerva
RD 24 abr 2026