Novel nanoparticles made from amphiphilic perfluoroalkyl α-cyclodextrin derivatives: Preparation, characterization and application to the transport of acyclovir
Novel nanoparticles made from amphiphilic perfluoroalkyl α-cyclodextrin derivatives: Preparation, characterization and application to the transport of acyclovir
复制标题
DOI：
10.1016/j.ijpharm.2009.04.004
复制
发表时间：
2009-06-22
影响因子：
5.8
通讯作者：
Parrot-Lopez, Helene
中科院分区：
文献类型：
--
作者：
Ghera, Bernard Bertino;Perret, Florent;Parrot-Lopez, Helene
研究了含氟两亲性α-环糊精hexakis[6-deoxy-6-(3-perfluoroalkylpropanethio)-2，3-di-O-methyl]-alpha-cyclodextrin及其碳氢化合物类似物纳米粒水悬浮液的制备方法。考察了阿昔洛韦与改性α-环糊精的络合作用、包封率和释药曲线，评价了纳米粒在药物传递方面的性能。对有机溶剂(乙醇)和环糊精浓度(0.4 mM)进行了精心选择。按优化条件制备的新型两亲性α-环糊精衍生物的平均直径为100 nm(含氟衍生物)和150 nm(烃类似物)。停职至少9个月是稳定的。经UV/Vis光谱和电喷雾电离质谱仪测定，阿昔洛韦形成化学计量比为1：1的包合物，其稳定常数在乙醇中为700moL L-1到4000molL-1。采用“高载药量”法制备阿昔洛韦纳米粒，包封率接近40%，包封率达到满意水平。基于含氟化合物的纳米粒将药物的释放延迟长达3小时，几乎没有初始的突释。含氟的两亲性α-环糊精以纳米球的形式自组装，包裹了阿昔洛韦并允许持续释放，显示了它们在药物释放方面的应用潜力。(C)2009爱思唯尔B.V.保留所有权利。
The preparation of aqueous suspensions of nanoparticles of the fluorinated amphiphilic alpha-cyclodextrins hexakis[6-deoxy-6-(3-perfluoroalkylpropanethio)-2,3-di-O-methyl]-alpha-cyclodextrin and their hydrocarbon analogues was studied. The complexation of acyclovir by modified alpha-cyclodextrin, the encapsulation efficiency and release profile were measured as an assessment of the properties of such nanoparticles regarding drug delivery applications.Stable aqueous suspensions of nanoparticles were prepared using nanoprecipitation method without using surface-active agent. The organic solvent (ethanol) and cyclodextrin concentration (0.4 mM) were carefully selected. The nanoparticles prepared from these new amphiphilic alpha-cyclodextrin derivatives according to optimized conditions have an average diameter of 100 nm for fluorinated derivatives and 150 nm for hydrocarbon analogues. Suspensions were stable over at least 9 months. Acyclovir forms inclusion complexes of 1:1 stoichiometry and high stability constants (from 700 mol L-1 to 4000 mol L-1 in ethanol) as assessed from UV/vis spectroscopy and Electrospray Ionization Mass Spectroscopy. Satisfactory loading of acyclovir inside the nanoparticles was achieved according to the "highly loaded" preparation method (encapsulation efficiency approximate to 40%). Nanoparticles based on the fluorinated compounds delayed the drug release up to 3 h with little initial burst release.Fluorinated amphiphilic alpha-cyclodextrins self-assemble in the form of nanospheres that encapsulate acyclovir and allow sustained release, showing their potential for applications to drug delivery. (C) 2009 Elsevier B.V. All rights reserved.