Ginevra F, Biffanti S, Pagnan A, Biolo R, Reddi E, Jori G
Department of Biology, University of Padova, Italy.
Cancer Lett. 1990 Jan;49(1):59-65. doi: 10.1016/0304-3835(90)90139-o.
Zn-phthalocyanine (Zn-Pc) incorporated into liposomes of different phospholipids has been incubated in vitro with human serum and administered i.v. to rabbits. In both cases, chromatographic and density gradient ultracentrifugation studies indicate that Zn-Pc is almost exclusively bound by the 3 major lipoprotein components of the plasma (VLDL, LDL and HDL). The amounts of Zn-Pc recovered from the different lipoprotein fractions reflect their relative concentration in the serum. The presence of 20% moles of cholesterol in liposomes of dipalmitoyl phosphatidylcholine (DPPC) optimizes the release of Zn-Pc to LDL. This fact is important for enhancing the selectivity of drug delivery to tumors since LDL display a preferential interaction with neoplastic cells.
将掺入不同磷脂脂质体中的锌酞菁（Zn-Pc）在体外与人血清一起孵育，并静脉注射给兔子。在这两种情况下，色谱和密度梯度超速离心研究表明，Zn-Pc几乎完全与血浆中的3种主要脂蛋白成分（极低密度脂蛋白、低密度脂蛋白和高密度脂蛋白）结合。从不同脂蛋白组分中回收的Zn-Pc量反映了它们在血清中的相对浓度。在二棕榈酰磷脂酰胆碱（DPPC）脂质体中存在20%摩尔的胆固醇可优化Zn-Pc向低密度脂蛋白的释放。这一事实对于提高药物向肿瘤的递送选择性很重要，因为低密度脂蛋白与肿瘤细胞表现出优先相互作用。
