title: Immunosuppressive Activity of Size-Controlled PEG-PLGA Nanoparticles Containing Encapsulated Cyclosporine A.
abstract: We encapsulated cyclosporine A (CsA) in poly(ethylene glycol)-b-poly(d,l-lactide-co-glycolide) (PEG-PLGA) nanoparticles (NPs) by nanoprecipitation of CsA and PEG-PLGA. The resulting CsA/PEG-PLGA-NPs were <100 nm in diameter with a narrow particle size distribution. The NP size could be controlled by tuning the polymer concentration, solvent, or water/solvent ratio during formulation. The PEGylated NPs maintained non-aggregated in salt solution. Solid NPs lyoprotected with bovine serum albumin were prepared for the convenience of storage and transportation. The release kinetics of CsA (55.6% released on Day 1) showed potential for maintaining therapeutic CsA concentrations in vivo. In T-cell assays, both free CsA and CsA/PEG-PLGA-NPs suppressed T-cell proliferation and production of inflammatory cytokines dose dependently. In a mixed lymphocyte reaction assay, the IC(50) values for free CsA and CsA/PEG-PLGA-NPs were found to be 30 and 35 ng/mL, respectively. This nanoparticulate CsA delivery technology constitutes a strong basis for future targeted delivery of immunosuppressive drugs with improved efficiency and potentially reduced toxicity.
authors.affiliation: Department of Materials Science and Engineering, University of Illinois at Urbana-Champaign, Urbana, IL 61801, USA.
authors.forename: Li
authors.initials: L
authors.lastname: Tang
authors.forename: Jamil
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authors.lastname: Azzi
authors.forename: Mincheol
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authors.lastname: Kwon
authors.forename: Marwan
authors.initials: M
authors.lastname: Mounayar
authors.forename: Rong
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authors.lastname: Tong
authors.forename: Qian
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authors.lastname: Yin
authors.forename: Robert
authors.initials: R
authors.lastname: Moore
authors.forename: Nikolaos
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authors.lastname: Skartsis
authors.forename: Timothy M
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authors.lastname: Fan
authors.forename: Reza
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authors.lastname: Abdi
authors.forename: Jianjun
authors.initials: J
authors.lastname: Cheng