Trotta Michele, Pattarino Franco, Ignoni Terenzio
Dipartimento di Scienza e Tecnologia del Farmaco, Università di Torino, Turin, Italy.
Eur J Pharm Biopharm. 2002 Mar;53(2):203-8. doi: 10.1016/s0939-6411(01)00230-2.
Lipid emulsion particles containing 10% of medium chain triglycerides were prepared using 2% w/w of a mixture 1:1 w/w of purified soya phosphatidylcholine and 2-hexanoyl phosphatidylcholine as emulsifier mixture, for use as drug carriers. The mean droplet sizes of emulsions, prepared using an Ultra Turrax or a high-pressure homogenizer, were about 288 and 158 nm, respectively, compared with 380 and 268 nm for emulsions containing lecithin, or 325 and 240 nm for those containing 6-phosphatidylcholine. The stability of the emulsions, determined by monitoring the decrease of a lipophilic marker at a specified level within the emulsion, and observing coalescence over time, was also greatly increased using the emulsifier mixture. The emulsion stability did not notably change in the presence of a model destabilizing drug, indomethacin. The use of a second hydrophilic surfactant to adjust the packing properties of the lecithin at the oil-water interface provided an increase in the stability of lipid emulsions, and this may be of importance in the formulation of drug delivery systems.
使用2%(w/w)的纯化大豆磷脂酰胆碱和2-己酰基磷脂酰胆碱按1:1(w/w)混合的混合物作为乳化剂混合物,制备了含有10%中链甘油三酯的脂质乳剂颗粒,用作药物载体。使用超高速均质器或高压均质器制备的乳剂的平均液滴尺寸分别约为288和158纳米,相比之下,含卵磷脂的乳剂为380和268纳米,含6-磷脂酰胆碱的乳剂为325和240纳米。通过监测乳剂中特定水平的亲脂性标记物的减少以及观察随时间的聚结来确定乳剂的稳定性,使用该乳化剂混合物时稳定性也大大提高。在存在模型去稳定药物吲哚美辛的情况下,乳剂稳定性没有明显变化。使用第二种亲水性表面活性剂来调节卵磷脂在油水界面的堆积性质可提高脂质乳剂的稳定性,这在药物递送系统的制剂中可能很重要。