title: Novel nanoemulsion based lipid nanosystems for favorable in vitro and in vivo characteristics of curcumin.
abstract: The goal of this study was to assess the enhanced elementary characteristics, in vitro release, anti-cancer cytotoxicity, in situ absorption and in vivo bioavailability of a novel nanoemulsion based lipid nanosystems containing curcumin (CNELNs) when administered orally. The CNELNs were first fabricated by loading water-in-oil nanoemulsions into lipid nanosystems using a nanoemulsion-film dispersion-sonication method. The gastro-intestinal absorption, in vitro release and in vivo kinetic property of CNELNs were investigated using an in situ perfusion method, a dialysis method and a concentration-time curve based method, respectively. The inhibitory effects of CNELNs on human lung cancer A549 cell growth were determined using MTT assay. The absorption constants and effective permeabilities of CNELNs in different gastro-intestinal tracts increased 2.29-4.04 times and 4.06-8.27 times that of curcumin (CUR), respectively. The relative bioavailability of CNELNs to free CUR was 733.59%. CNELNs inhibited A549 growth in a dose- and time-dependent manner. CNELNs markedly improved the oral bioavailability of CUR which was probably due to the increased gastro-intestinal absorption. CNELNs had stronger inhibitory effects on the viabilities of A549 cells than that of free CUR. CNELNs might be promising nanosystems for oral delivery of CUR to satisfy clinical requirements.
authors.affiliation: Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China.
authors.forename: Kun
authors.initials: K
authors.lastname: Wan
authors.affiliation: Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China.
authors.forename: Lili
authors.initials: L
authors.lastname: Sun
authors.affiliation: Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China.
authors.forename: Xueyuan
authors.initials: X
authors.lastname: Hu
authors.affiliation: Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China.
authors.forename: Zijun
authors.initials: Z
authors.lastname: Yan
authors.affiliation: Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China.
authors.forename: Yonghong
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China.
authors.forename: Xue
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Chongqing Research Center for Pharmaceutical Engineering, Chongqing Medical University, Chongqing 400016, PR China. Electronic address: zjqrae01@163.com.
authors.forename: Jingqing
authors.initials: J
authors.lastname: Zhang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003474:Curcumin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004655:Emulsions; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects; D008055:Lipids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D017207:Rats, Sprague-Dawley
chemical_list: D000970:Antineoplastic Agents; D004655:Emulsions; D008055:Lipids; D003474:Curcumin
keywords: Anti-cancer cytotoxicity; Characteristics; In situ absorption; In vivo kinetic property; Nanoemulsion based lipid nanosystems