Ishii F, Nagasaka Y, Ogata H
Department of Physical Pharmaceutics and Biopharmaceutics, Meiji College of Pharmacy, Tokyo, Japan.
J Pharm Sci. 1989 Apr;78(4):303-6. doi: 10.1002/jps.2600780408.
The degree of hemolysis caused by the interaction between erythrocytes from various animals and emulsions stabilized with various lecithins was evaluated as a measure of the safety of emulsions for drug carriers. The stability of the emulsions was estimated using the gradient of the slope derived from the direct linear correlation between the percentage hemolysis and the phosphatidylcholine (PC) content of the erythrocyte membrane. When members of the egg lecithin (EPC) series were used as emulsifiers of emulsions, the percentage hemolysis increased as the PC content of the erythrocyte membrane increased and as the sphingomyelin (SM) content of the erythrocyte membrane decreased. Lysolecithin, a contaminant present in the emulsifying agent of emulsions, did not have any significant influence on the hemolysis of erythrocytes. These experimental findings show that the hemolysis caused by interaction between emulsions and erythrocytes was dependent on the PC content of both the emulsifying agent used and the erythrocyte membrane, and that the SM present in the erythrocyte membrane was an essential component for the stability of erythrocytes against emulsion-induced hemolysis.
评估了来自各种动物的红细胞与用各种卵磷脂稳定的乳剂之间相互作用所引起的溶血程度,以此作为乳剂作为药物载体安全性的一种衡量指标。利用溶血百分比与红细胞膜磷脂酰胆碱(PC)含量之间直接线性相关得出的斜率梯度来估计乳剂的稳定性。当使用卵磷脂(EPC)系列成员作为乳剂的乳化剂时,溶血百分比随着红细胞膜PC含量的增加以及红细胞膜鞘磷脂(SM)含量的降低而增加。溶血卵磷脂是乳剂乳化剂中存在的一种污染物,对红细胞的溶血没有任何显著影响。这些实验结果表明,乳剂与红细胞之间相互作用引起的溶血取决于所用乳化剂和红细胞膜的PC含量,并且红细胞膜中存在的SM是红细胞抵抗乳剂诱导溶血稳定性的重要成分。