title: In Vitro Study of a Liposomal Curcumin Formulation (Lipocurc™): Toxicity and Biological Activity in Synovial Fibroblasts and Macrophages.
abstract: OBJECTIVE
  The polyphenol curcumin is produced in the rhizome of Curcuma longa and exhibits potent anti-inflammatory, antioxidant, and chemopreventive activities. Due to the fact that curcumin is poorly soluble in water, many delivery systems have been developed to improve its solubility and bioavailability achieving optimum therapeutic application. In this study, we evaluated the biological effects of a liposomal curcumin formulation (Lipocurc™) on human synovial fibroblasts (SW982) and mouse macrophages (RAW264).
  
  
  METHODS
  Cellular uptake of liposomes was studied using calcein-loaded liposomes. Effects of Lipocurc™ on cell viability and proliferation were determined with Celltox green cytotoxicity assay and 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) assay, respectively. To induce cytokine/chemokine expression, the cells were stimulated with interleukin (IL)1β or lipopolysaccharide (LPS). The release of IL6, IL8, and tumor necrosis factor-alpha (TNFα) was quantified by enzyme-linked immunosorbent assay (ELISA).
  
  
  RESULTS
  Data showed that the liposomal curcumin formulation Lipocurc™ was significantly less toxic to synovial fibroblasts and macrophages compared to non-encapsulated, free curcumin. Furthermore, Lipocurc™ effectively reduced pro-inflammatory cytokine/chemokine expression in synovial fibroblasts as well as in macrophages without affecting cell viability, suggesting that this curcumin nanoformulation might be a promising tool for the treatment of inflammatory diseases.
authors.affiliation: Department for Degenerative Joint Diseases, Ludwig Boltzmann Cluster for Arthritis and Rehabilitation, Vienna, Austria burkhard.kloesch@gmx.at.
authors.forename: Burkhard
authors.initials: B
authors.lastname: Kloesch
authors.affiliation: Department for Degenerative Joint Diseases, Ludwig Boltzmann Cluster for Arthritis and Rehabilitation, Vienna, Austria.
authors.forename: Lukas
authors.initials: L
authors.lastname: Gober
authors.affiliation: Department for Degenerative Joint Diseases, Ludwig Boltzmann Cluster for Arthritis and Rehabilitation, Vienna, Austria.
authors.forename: Silvia
authors.initials: S
authors.lastname: Loebsch
authors.affiliation: Polymun Scientific GmbH, Klosterneuburg, Austria.
authors.forename: Brigitta
authors.initials: B
authors.lastname: Vcelar
authors.affiliation: Sign Path Pharma, Inc., Quakertown, PA, U.S.A.
authors.forename: Lawrence
authors.initials: L
authors.lastname: Helson
authors.affiliation: Department for Degenerative Joint Diseases, Ludwig Boltzmann Cluster for Arthritis and Rehabilitation, Vienna, Austria Division of Rheumatology, Department for Internal Medicine III, Medical University of Vienna, Vienna, Austria.
authors.forename: Guenter
authors.initials: G
authors.lastname: Steiner
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects*; D003474:Curcumin / Q000494:pharmacology*; D016207:Cytokines / Q000378:metabolism; D004797:Enzyme-Linked Immunosorbent Assay; D005347:Fibroblasts / Q000187:drug effects / Q000378:metabolism / Q000473:pathology*; D006801:Humans; D066298:In Vitro Techniques; D008070:Lipopolysaccharides / Q000494:pharmacology; D008081:Liposomes / Q000737:chemistry*; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism / Q000473:pathology*; D051379:Mice; D016328:NF-kappa B / Q000378:metabolism; D013582:Synovial Fluid / Q000737:chemistry*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D016207:Cytokines; D008070:Lipopolysaccharides; D008081:Liposomes; D016328:NF-kappa B; D003474:Curcumin
keywords: Liposomal curcumin; inflammation; toxicity