title: Targeted delivery of NK007 to macrophages to treat colitis.
abstract: Macrophages are important therapeutic targets for various disorders, including infectious diseases, inflammatory diseases, metabolic diseases, and cancer. In this study, we report a novel oral delivery system for the targeted delivery of anti-inflammatory therapeutics to macrophages. Using this formulation, the model drug tylophorine malate (NK007) was tightly incorporated inside beta-glucan particle shells by the formation of colloidal particles with chitosan, tripolyphosphate, and alginate via electrostatic interactions. This formulation specifically delivered NK007 to macrophages in vivo after oral gavage and effectively cured colitis in the dextran sulfate sodium-induced murine colitis model, highlighting the utility of beta-glucan particles as an oral anti-inflammation drug delivery system by targeting macrophages. In this work, NK007 was selected as the model drug. However, this novel oral carrier system has the potential to be applied as a platform for the treatment of many other diseases for which macrophages are the therapeutic targets.
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
authors.forename: Siming
authors.initials: S
authors.lastname: Chen
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
authors.forename: Jin
authors.initials: J
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
authors.forename: Hao
authors.initials: H
authors.lastname: Cheng
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
authors.forename: Wenjun
authors.initials: W
authors.lastname: Guo
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
authors.forename: Min
authors.initials: M
authors.lastname: Yu
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhao
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
authors.forename: Zhenzhou
authors.initials: Z
authors.lastname: Wu
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
authors.forename: Liqing
authors.initials: L
authors.lastname: Zhao
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
authors.forename: Zhinan
authors.initials: Z
authors.lastname: Yin
authors.affiliation: State Key Laboratory of Medicinal Chemical Biology, College of Life Sciences, Nankai University, Tianjin, 300071, P. R. China.
authors.forename: Zhangyong
authors.initials: Z
authors.lastname: Hong
mesh_terms: D000464:Alginates / Q000737:chemistry; D000470:Alkaloids / Q000737:chemistry; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D048271:Chitosan / Q000737:chemistry; D003092:Colitis / Q000188:drug therapy*; D003106:Colon / Q000187:drug effects; D016264:Dextran Sulfate / Q000737:chemistry; D004195:Disease Models, Animal; D016503:Drug Delivery Systems / Q000379:methods; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D007212:Indolizines / Q000737:chemistry; D008264:Macrophages / Q000187:drug effects*; D051379:Mice; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000737:chemistry*; D010616:Phenanthrenes / Q000737:chemistry
chemical_list: D000464:Alginates; D000470:Alkaloids; D000893:Anti-Inflammatory Agents; D006603:Hexuronic Acids; D007212:Indolizines; D004364:Pharmaceutical Preparations; D010616:Phenanthrenes; D020723:Glucuronic Acid; D048271:Chitosan; D016264:Dextran Sulfate; C004218:tylophorine
keywords: biodegradable polymers; colitis; colonic drug delivery; encapsulation; glucan particle; inflammatory cytokine; macrophage; oral absorption; targeted drug delivery