Zhiqiang Tian1, Qin Yu1, Yunchang Xie1, Fengqian Li2, Yi Lu1, Xiaochun Dong1, Weili Zhao1,3, Jianping Qi4, Wei Wu5. 1. School of Pharmacy, Key Laboratory of Smart Drug Delivery of MOE and PLA, Fudan University, Shanghai, 201203, China. 2. Department of Pharmacy, Shanghai Xuhui Dahua Hospital, Shanghai, China. 3. Key Laboratory for Special Functional Materials of the Ministry of Education, Henan University, Kaifeng, China. 4. School of Pharmacy, Key Laboratory of Smart Drug Delivery of MOE and PLA, Fudan University, Shanghai, 201203, China. qijianping@fudan.edu.cn. 5. School of Pharmacy, Key Laboratory of Smart Drug Delivery of MOE and PLA, Fudan University, Shanghai, 201203, China. wuwei@shmu.edu.cn.
Abstract
PURPOSE: To achieve controlled release of integral nanoparticles by the osmotic pump strategy using nanostructured lipid carriers (NLCs) as model nanoparticles. METHODS: 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. RESULTS: 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. CONCLUSION: Controlled release of integral NLCs is achieved by the osmotic pump strategy.
PURPOSE: To achieve controlled release of integral nanoparticles by the osmotic pump strategy using nanostructured lipid carriers (NLCs) as model nanoparticles. METHODS: 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. RESULTS: 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. CONCLUSION: Controlled release of integral NLCs is achieved by the osmotic pump strategy.
Authors: Ortensia I Parisi; Marco Fiorillo; Luca Scrivano; Maria S Sinicropi; Vincenza Dolce; Domenico Iacopetta; Francesco Puoci; Anna R Cappello Journal: Biomacromolecules Date: 2015-09-17 Impact factor: 6.988
Authors: Maria Manuela Gaspar; Susana Calado; Joana Pereira; Helena Ferronha; Ivone Correia; Helena Castro; Ana M Tomás; Maria Eugénia Meirinhos Cruz Journal: Nanomedicine Date: 2015-07-11 Impact factor: 5.307