title: Smart conjugated polymer nanocarrier for healthy weight loss by negative feedback regulation of lipase activity.
abstract: Healthy weight loss represents a real challenge when obesity is increasing in prevalence. Herein, we report a conjugated polymer nanocarrier for smart deactivation of lipase and thus balancing calorie intake. After oral administration, the nanocarrier is sensitive to lipase in the digestive tract and releases orlistat, which deactivates the enzyme and inhibits fat digestion. It also creates negative feedback to control the release of itself. The nanocarrier smartly regulates activity of the lipase cyclically varied between high and low levels. In spite of high fat diet intervention, obese mice receiving a single dose of the nanocarrier lose weight over eight days, whereas a control group continues the tendency to gain weight. Daily intragastric administration of the nanocarrier leads to lower weight of livers or fat pads, smaller adipocyte size, and lower total cholesterol level than that of the control group. Near-infrared fluorescence of the nanocarrier reveals its biodistribution.
authors.affiliation: Department of Polymer Science & Engineering and Key Laboratory of High Performance Polymer Materials & Technology of MOE, School of Chemistry & Chemical Engineering, Nanjing University, Nanjing 210093, P. R. China. qdshen@nju.edu.cn.
authors.forename: Yu-Lei
authors.initials: YL
authors.lastname: Chen
authors.forename: Sha
authors.initials: S
authors.lastname: Zhu
authors.forename: Lei
authors.initials: L
authors.lastname: Zhang
authors.forename: Pei-Jian
authors.initials: PJ
authors.lastname: Feng
authors.forename: Xi-Kuang
authors.initials: XK
authors.lastname: Yao
authors.forename: Cheng-Gen
authors.initials: CG
authors.lastname: Qian
authors.forename: Can
authors.initials: C
authors.lastname: Zhang
authors.forename: Xi-Qun
authors.initials: XQ
authors.lastname: Jiang
authors.forename: Qun-Dong
authors.initials: QD
authors.lastname: Shen
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000737:chemistry / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry / Q000494:pharmacology; D007783:Lactones / Q000737:chemistry / Q000494:pharmacology; D008049:Lipase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D053758:Nanoparticles / Q000737:chemistry*; D000077403:Orlistat; D015431:Weight Loss / Q000187:drug effects*
chemical_list: D019440:Anti-Obesity Agents; D004337:Drug Carriers; D007783:Lactones; D000077403:Orlistat; D008049:Lipase