Choisnard L, Gèze A, Yaméogo B G J, Putaux J-L, Wouessidjewe D
Université Joseph-Fourier, UFR de pharmacie ICMG FR-2607 - DPM UMR UJF/CNRS 5063, 470 rue de la Chimie, BP 53, F-38041, Grenoble cedex 9, France.
Int J Pharm. 2007 Nov 1;344(1-2):26-32. doi: 10.1016/j.ijpharm.2007.06.026. Epub 2007 Jun 23.
Various beta-cyclodextrin (beta-CD) fatty esters with different chain lengths (C4-C14) were synthesised by transesterification of beta-cyclodextrin by vinyl fatty ester using thermolysin in DMSO. For each cyclodextrin derivatives, two batches of synthesis were realized. The ability of these derivatives to form nano-organized systems was investigated through the solvent displacement technique. During the formulation step, the effects of the initial concentration of beta-CD fatty esters in the organic phase and that of the final volume of the aqueous non-solvent phase were studied. Except for the beta-CD C4 ester, the transesterified beta-CD derivatives led to measurable nanoparticles. Cryo-electron microscopy images showed a significant morphological variability. Spherical, rod-like or more irregularly-shaped nano-objects were observed with either matricial or lamellar structures. A statistical analysis by a two-way ANOVA was computed for each class of beta-cyclodextrin esters in order to determine the effects of batch and formulation on the final size of nanoparticles.
使用嗜热菌蛋白酶在二甲基亚砜（DMSO）中通过β-环糊精与乙烯基脂肪酸酯的酯交换反应合成了具有不同链长（C4 - C14）的各种β-环糊精（β-CD）脂肪酸酯。对于每种环糊精衍生物，进行了两批合成。通过溶剂置换技术研究了这些衍生物形成纳米有序体系的能力。在制剂步骤中，研究了有机相中β-CD脂肪酸酯的初始浓度和非水相最终体积的影响。除了β-CD C4酯外，酯交换后的β-CD衍生物形成了可测量的纳米颗粒。冷冻电子显微镜图像显示出显著的形态变异性。观察到具有基质或层状结构的球形、棒状或形状更不规则的纳米物体。为了确定批次和制剂对纳米颗粒最终尺寸的影响，对每类β-环糊精酯进行了双向方差分析的统计分析。
