title: Controlling Release of Integral Lipid Nanoparticles Based on Osmotic Pump Technology.
abstract: To achieve controlled release of integral nanoparticles by the osmotic pump strategy using nanostructured lipid carriers (NLCs) as model nanoparticles.
  
  
  
  NLCs was prepared by a hot-homogenization method, transformed into powder by lyophilization, and formulated into osmotic pump tablets (OPTs). Release of integral NLCs was visualized by live imaging after labeling with a water-quenching fluorescent probe. Effects of formulation variables on in vitro release characteristics were evaluated by measuring the model drug fenofibrate. Pharmacokinetics were studied in beagle dogs using the core tablet and a micronized fenofibrate formulation as references.
  
  
  
  NLCs are released through the release orifices of the OPTs as integral nanoparticles. Near zero-order kinetics can be achieved by optimizing the influencing variables. After oral administration, decreased C max and steady drug levels for as long as over 24 h are observed. NLC-OPTs show an oral bioavailability of the model drug fenofibrate similar to that of the core tablets, which is about 1.75 folds that of a fast-release formulation.
  
  
  
  Controlled release of integral NLCs is achieved by the osmotic pump strategy.
authors.affiliation: School of Pharmacy, Key Laboratory of Smart Drug Delivery of MOE and PLA, Fudan University, Shanghai, 201203, China.
authors.forename: Zhiqiang
authors.initials: Z
authors.lastname: Tian
authors.affiliation: School of Pharmacy, Key Laboratory of Smart Drug Delivery of MOE and PLA, Fudan University, Shanghai, 201203, China.
authors.forename: Qin
authors.initials: Q
authors.lastname: Yu
authors.affiliation: School of Pharmacy, Key Laboratory of Smart Drug Delivery of MOE and PLA, Fudan University, Shanghai, 201203, China.
authors.forename: Yunchang
authors.initials: Y
authors.lastname: Xie
authors.affiliation: Department of Pharmacy, Shanghai Xuhui Dahua Hospital, Shanghai, China.
authors.forename: Fengqian
authors.initials: F
authors.lastname: Li
authors.affiliation: School of Pharmacy, Key Laboratory of Smart Drug Delivery of MOE and PLA, Fudan University, Shanghai, 201203, China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Lu
authors.affiliation: School of Pharmacy, Key Laboratory of Smart Drug Delivery of MOE and PLA, Fudan University, Shanghai, 201203, China.
authors.forename: Xiaochun
authors.initials: X
authors.lastname: Dong
authors.affiliation: School of Pharmacy, Key Laboratory of Smart Drug Delivery of MOE and PLA, Fudan University, Shanghai, 201203, China.|Key Laboratory for Special Functional Materials of the Ministry of Education, Henan University, Kaifeng, China.
authors.forename: Weili
authors.initials: W
authors.lastname: Zhao
authors.affiliation: School of Pharmacy, Key Laboratory of Smart Drug Delivery of MOE and PLA, Fudan University, Shanghai, 201203, China. qijianping@fudan.edu.cn.
authors.forename: Jianping
authors.initials: J
authors.lastname: Qi
authors.affiliation: School of Pharmacy, Key Laboratory of Smart Drug Delivery of MOE and PLA, Fudan University, Shanghai, 201203, China. wuwei@shmu.edu.cn.
authors.forename: Wei
authors.initials: W
authors.lastname: Wu
mesh_terms: D000818:Animals; D018592:Cross-Over Studies; D004285:Dogs; D016503:Drug Delivery Systems / Q000379:methods*; D011345:Fenofibrate / Q000008:administration & dosage / Q000493:pharmacokinetics; D015918:Infusion Pumps, Implantable; D008055:Lipids / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D053758:Nanoparticles / Q000008:administration & dosage* / Q000378:metabolism*; D009997:Osmotic Pressure
chemical_list: D008055:Lipids; D011345:Fenofibrate
keywords: controlled release; nanoparticles; nanostructured lipid carriers; oral drug delivery; osmotic pump