Vuaridel-Bonanomi E S, Weder H G
School of Pharmacy, Department of Physical Pharmacy, Swiss Federal Institute of Technology (ETH), Zürich, Switzerland.
J Microencapsul. 1991 Apr-Jun;8(2):203-14. doi: 10.3109/02652049109071488.
Artificial chylomicron remnants were investigated as a new drug carrier system for the targeting of hepatic parenchymal cells. The emulsions presented here are similar in particle size and composition to natural lipoproteins. The preparations contained triolein, phospholipid, cholesterol and cholesteryl oleate. Egg yolk lecithin was either used to form multilamellar or unilamellar liposomes or it was incorporated into a lipid film prior to emulsification. Typically the lipid film contained triolein, cholesterol and cholesteryl oleate. When multilamellar liposomes were used however, cholesterol and cholesteryl oleate were incorporated into the vesicles. The emulsions were prepared by ultrasonication or by means of a microemulsifier. The unilamellar liposomes used with the microemulsifier yielded the best particle distribution, i.e. in the range of 40-60 as determined by quasi-elastic light scattering. The advantage of the method results from the complete emulsification of the components. The particle size remained unchanged during storage, although flocculation was observed. The results show that the synthesis of artificial chylomicron remnants in a microemulsifier is possible and reproducible.
人工乳糜微粒残粒作为一种用于靶向肝实质细胞的新型药物载体系统进行了研究。此处呈现的乳液在粒径和组成上与天然脂蛋白相似。制剂包含三油酸甘油酯、磷脂、胆固醇和油酸胆固醇酯。蛋黄卵磷脂要么用于形成多层或单层脂质体,要么在乳化前被掺入脂质膜中。通常脂质膜包含三油酸甘油酯、胆固醇和油酸胆固醇酯。然而,当使用多层脂质体时,胆固醇和油酸胆固醇酯被掺入囊泡中。乳液通过超声处理或借助微乳化剂制备。与微乳化剂一起使用的单层脂质体产生了最佳的颗粒分布,即通过准弹性光散射测定在40 - 60范围内。该方法的优点源于组分的完全乳化。尽管观察到絮凝现象,但在储存期间粒径保持不变。结果表明,在微乳化剂中合成人工乳糜微粒残粒是可行且可重复的。