Drug loading to lipid-based cationic nanoparticles

被引:15
作者
Cavalcanti, LP
Konovalov, O
Torriani, IL
Haas, H
机构
[1] European Synchrotron Radiat Facil, F-38043 Grenoble, France
[2] UNICAMP, LNLS, Campinas, SP, Brazil
[3] Munich Biotech AG, Neuried, Germany
关键词
nanoparticles; liposomes; X ray diffraction; GID; cancer; drug targeting; paclitaxel;
D O I
10.1016/j.nimb.2005.06.065
中图分类号
TH7 [仪器、仪表];
学科分类号
0804 ; 080401 ; 081102 ;
摘要
Lipid-based cationic nanoparticles are a new promising option for tumor therapy, because they display enhanced binding and uptake at the neo-angiogenic endothelial cells, which a tumor needs for its nutrition and growth. By loading suitable cytotoxic compounds to the cationic carrier, the tumor endothelial and consequently also the tumor itself can be destroyed. For the development of such novel anti-tumor agents, the control of drug loading and drug release from the carrier matrix is essential. We have studied the incorporation of the hydrophobic anti-cancer agent Paclitaxel (PXL) into a variety of lipid matrices by X-Ray reflectivity measurements. Liposome suspensions from cationic and zwitterionic lipids, comprising different molar fractions of Paclitaxel, were deposited on planar glass substrates. After drying at controlled humidity, well ordered, oriented multilayer stacks were obtained, as proven by the presence of bilayer Bragg peaks to several orders in the reflectivity curves. The presence of the drug induced a decrease of the lipid bilayer spacing, and with an excess of drug, also Bragg peaks of drug crystals could be observed. From the results, insight into the solubility of Paclitaxel in the model membranes was obtained and a structural model of the organization of the drug in the membrane was derived. Results from subsequent pressure/area-isotherm and grazing incidence diffraction (GID) measurements performed with drug/lipid Langmuir monolayers were in accordance with these conjectures. (c) 2005 Elsevier B.V. All rights reserved.
引用
收藏
页码:290 / 293
页数:4
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