在传代培养的HeLa细胞上观察了叶酸对脂质体靶向摄取功能的影响。将内含钙黄绿素的叶酸.脂质体和脂质体分别加入HeLa细胞中培养,并以荧光法检测细胞摄取量。共同培养4h,细胞摄取叶酸一脂质体量为脂质体4倍以上,在0.45mg· mL-1时达饱和;过量游离叶酸竞争抑制细胞对叶酸-脂质体的摄取;磷脂酶D或磷脂酰肌醇特异性磷脂酶C通过影响叶酸受体而抑制细胞对叶酸-脂质体的摄取。因此,HeLa细胞主要通过叶酸受体途径介导摄取叶酸-脂质体:叶酸受体高表达或高活性细胞摄取叶酸-脂质体的能力较未接叶酸的脂质体显著提高。
Effect of folio acid on delivery of liposomes was examined using cultured HeLa cells. Folateliposomes encapsulating calcein and liposomes were cultured with HeLa cells respectively. Liposomes taken up bycells were measured by a fluorescence spectrophotometer. The cell fluorescence increased slowly at the 4 h timepoint, and the saturated folate-liposome concentration was 0.45 mg.mL~-1. The binding of folate-liposomes to HeLacells could be competitively inhibited by excess free folate. Enzyme phospholipase D (PLD) or phosphatidylinositolspecific phospholipase C (PIPLC) influenced liposome uptake via folate receptor. Folate targeting improved the specificity of liposomes for cells which overexpressed the folate receptors.