Gattefossé SAS, 36 chemin de Genas, 69804 Saint-Priest cedex, France.
Laboratoire NS3E, UMR 3208 ISL-CNRS-UNISTRA, 5 rue du Général Cassagnou, 68301 Saint-Louis, France.
Eur J Pharm Sci. 2018 Jan 1;111:91-95. doi: 10.1016/j.ejps.2017.09.049. Epub 2017 Sep 29.
To evaluate the digestibility of Solid Lipid Nanoparticles (SLN) of glyceryl dibehenate prepared either with surfactants by ultrasonication or without surfactant by spray-flash evaporation.
SLN of glyceryl dibehenate (Compritol® 888 ATO) were produced by two processes: (i) high-shear homogenization with a solution of water-soluble surfactants followed by ultrasonication (ii) and Spray-Flash Evaporation (SFE) of the pure lipid. The digestibility of these nanoparticles was then tested by in vitro lipolysis using a pH-stat apparatus and the assay of glycerides by gel phase chromatography.
SLN of glyceryl dibehenate prepared by ultrasonication exhibited a mean particle size of 180nm and showed a limited digestion of the lipid excipient. SLN comprising only glyceryl dibehenate produced by SFE have a mean particle size between 235 and 411nm depending on process parameters. These nanoparticles were not digested by lipases. The presence of surfactant at the lipid/water interface of the SLN seems to be mandatory to allow the adsorption of the lipase and degradation of glyceryl behenate.
Glyceryl dibehenate as a solid particle - even as a SLN - is not digested by pancreatin during in vitro lipolysis test.
评估通过超声处理使用表面活性剂或不使用表面活性剂通过喷雾闪蒸蒸发制备的二硬脂酸甘油酯固体脂质纳米粒(SLN)的消化率。
通过两种方法制备二硬脂酸甘油酯(Compritol®888 ATO)的 SLN:(i)使用水溶性表面活性剂的溶液进行高剪切匀化,然后进行超声处理;(ii)纯脂质的喷雾闪蒸蒸发(SFE)。然后使用 pH -stat 仪器通过体外脂肪分解试验和凝胶相色谱法测定甘油酯来测试这些纳米粒子的消化率。
通过超声处理制备的二硬脂酸甘油酯 SLN 的平均粒径为 180nm,显示出对脂质赋形剂的有限消化。仅由 SFE 产生的包含二硬脂酸甘油酯的 SLN 的平均粒径在 235nm 至 411nm 之间,具体取决于工艺参数。这些纳米粒子不能被脂肪酶消化。在 SLN 的脂质/水界面处存在表面活性剂似乎是必需的,以允许脂肪酶的吸附和二硬脂酸甘油酯的降解。
在体外脂肪分解试验中,二硬脂酸甘油酯作为固体颗粒-即使是 SLN-也不会被胰蛋白酶消化。