文献类型：期刊文献

英文题名：Preparation and characterization of a nanostructured lipid carrier for a poorly soluble drug

作者：Chen, Yiyin[1,2,3];Yang, Xiaomin[1,2,3];Zhao, Lin[5];Almasy, Laszlo[6];Garamus, Vasil M.[4];Willumeit, Regine[4];Zou, Aihua[1,2,3]

机构：[1]E China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[2]E China Univ Sci & Technol, Shanghai Key Lab Funct Mat Chem, Shanghai 200237, Peoples R China;[3]E China Univ Sci & Technol, Inst Appl Chem, Shanghai 200237, Peoples R China;[4]Helmholtz Zentrum Geesthacht, Inst Mat Res, Ctr Mat & Coast Res, D-21502 Geesthacht, Germany;[5]Soochow Univ, Coll Med, Sch Radiat Med & Protect, Suzhou 215123, Peoples R China;[6]Wigner Res Ctr Phys, Inst Solid State Phys & Opt, H-1525 Budapest, Hungary

年份：2014

卷号：455

期号：1

起止页码：36

外文期刊名：COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS

收录：;EI(收录号：20142017717886);WOS:【SCI-EXPANDED(收录号:WOS:000337878400005)】；

基金：Aihua Zou gratefully acknowledges the support of this work by the Alexander von Humboldt Foundation. Lihui Zhou is acknowledged for help during TEM measurements. We gratefully acknowledge the support of this work by Chinese National Natural Science Foundation (201003047) and Fundamental Research Funds for the Central Universities. SANS measurements have been performed under support of the European Commission (Grant agreement N 283883-NMI3).

语种：英文

外文关键词：Nanostructured lipid carrier; Docetaxel; SANS; SAXS; Cytotoxicity

摘要：The aim of this study was to prepare a stable nanostructured lipid carrier (NLC) with biocompatible lipids and surfactants (Pluronic F68 and Cremophor EL) by high-pressure homogenization (HPH). Surface tension measurements were used to choose the suitable ratio between Pluronic F68 and Cremophor EL. Hydrophobic anticancer drug docetaxel (DTX) was used as an active pharmaceutical ingredient (API). The mean particle size of docetaxel loaded nanostructured lipid carrier (DTX-NLC), as determined by dynamic light scattering (DLS), was between 120 nm and 250 nm during the storage period of 30 days, with the entrapment efficiency decreasing from (60.5 +/- 5.0)% to (55.3 +/- 4.5)%, while zeta potential was slightly changed from (-43.19 +/- 3.6) mV to (-40.12 +/- 4.3) mV. Transmission electron microscopy (TEM) showed that some of DTX-NLCs have elongated shape. Small angle neutron scattering (SANS) demonstrated that DTX-NLC in solution contained dense core with perfectly smooth surface, while blank NLC had dense core but rough surface. The blank NLC and DTX-NLC showed cubic crystalline structure according to small angle X-ray scattering (SAXS). Wide angle X-ray diffraction (XRD) showed that adding of DTX increased the crystallinity of the NLC. Cytotoxicity was studied by MTT assay against Hela cells. The data suggested that blank NLC was biocompatible with HeLa cells while the DTX-NLC was more cytotoxic than pure DTX at the same drug concentration. DTX-NLC could be taken up into the cells more than pure DTX, which could be attributed to the better solubility of DTX after loading into NLC. (C) 2014 Elsevier B.V. All rights reserved.