title: Enhancement of Anti-Inflammatory Activity of Curcumin Using Phosphatidylserine-Containing Nanoparticles in Cultured Macrophages.
abstract: Macrophages are one kind of innate immune cells, and produce a variety of inflammatory cytokines in response to various stimuli, such as oxidized low density lipoprotein found in the pathogenesis of atherosclerosis. In this study, the effect of phosphatidylserine on anti-inflammatory activity of curcumin-loaded nanostructured lipid carriers was investigated using macrophage cultures. Different amounts of phosphatidylserine were used in the preparation of curcumin nanoparticles, their physicochemical properties and biocompatibilities were then compared. Cellular uptake of the nanoparticles was investigated using a confocal laser scanning microscope and flow cytometry analysis in order to determine the optimal phosphatidylserine concentration. In vitro anti-inflammatory activities were evaluated in macrophages to test whether curcumin and phosphatidylserine have interactive effects on macrophage lipid uptake behavior and anti-inflammatory responses. Here, we showed that macrophage uptake of phosphatidylserine-containing nanostructured lipid carriers increased with increasing amount of phosphatidylserine in the range of 0%-8%, and decreased when the phosphatidylserine molar ratio reached over 12%. curcumin-loaded nanostructured lipid carriers significantly inhibited lipid accumulation and pro-inflammatory factor production in cultured macrophages, and evidently promoted release of anti-inflammatory cytokines, when compared with curcumin or phosphatidylserine alone. These results suggest that the delivery system using PS-based nanoparticles has great potential for efficient delivery of drugs such as curcumin, specifically targeting macrophages and modulation of their anti-inflammatory functions.
authors.affiliation: State Key Laboratory of Military Stomatology &amp; National Clinical Research Center for Oral Diseases &amp; Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, 145 Changle West Road, Xi'an 710032, China. wjsydkq145@163.com.
authors.forename: Ji
authors.initials: J
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Military Stomatology &amp; National Clinical Research Center for Oral Diseases &amp; Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, 145 Changle West Road, Xi'an 710032, China. kangyuxia1030@163.com.
authors.forename: Yu-Xia
authors.initials: YX
authors.lastname: Kang
authors.affiliation: State Key Laboratory of Military Stomatology &amp; National Clinical Research Center for Oral Diseases &amp; Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, 145 Changle West Road, Xi'an 710032, China. 15691087927@163.com.
authors.forename: Wen
authors.initials: W
authors.lastname: Pan
authors.affiliation: State Key Laboratory of Military Stomatology &amp; National Clinical Research Center for Oral Diseases &amp; Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, 145 Changle West Road, Xi'an 710032, China. 15129627980@163.com.
authors.forename: Wan
authors.initials: W
authors.lastname: Lei
authors.affiliation: State Key Laboratory of Military Stomatology &amp; National Clinical Research Center for Oral Diseases &amp; Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, 145 Changle West Road, Xi'an 710032, China. bingelfeng@hotmail.com.
authors.forename: Bin
authors.initials: B
authors.lastname: Feng
authors.affiliation: State Key Laboratory of Military Stomatology &amp; National Clinical Research Center for Oral Diseases &amp; Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, 145 Changle West Road, Xi'an 710032, China. kqyyyjk@fmmu.edu.cn.
authors.forename: Xiao-Juan
authors.initials: XJ
authors.lastname: Wang
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D002478:Cells, Cultured; D003474:Curcumin / Q000494:pharmacology*; D016207:Cytokines / Q000235:genetics / Q000378:metabolism; D008264:Macrophages / Q000187:drug effects* / Q000378:metabolism; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010718:Phosphatidylserines / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000893:Anti-Inflammatory Agents; D016207:Cytokines; D010718:Phosphatidylserines; D003474:Curcumin
keywords: anti-inflammatory; curcumin; macrophages; nanostructured lipid carriers; phosphatidylserine