Kwon, MincheolFan, Timothy M.Cheng, JianjunTang, LiAzzi, JamilMounayar, MarwanYin, QianMoore, RobertSkartsis, NikolaosAbdi, RezaTong, Rong2013-02-262012Tang, Li, Jamil Azzi, Mincheol Kwon, Marwan Mounayar, Rong Tong, Qian Yin, Robert Moore, et al. 2012. Immunosuppressive activity of size-controlled PEG-PLGA nanoparticles containing encapsulated cyclosporine A. Journal of Transplantation 2012:896141.2090-0007http://nrs.harvard.edu/urn-3:HUL.InstRepos:10346974We 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.en-USJournal Article2013-02-2610.1155/2012/896141