Pantos Alexandros, Tsiourvas Dimitris, Paleos Constantinos M, Nounesis George
Institutes of Physical Chemistry and of Radioisotopes and Radiodiagnostic Products, NCSR Demokritos, 15310 Aghia Paraskevi, Attiki, Greece.
Langmuir. 2005 Jul 19;21(15):6696-702. doi: 10.1021/la050211n.
Unilamellar PC-based liposomes bearing a recognizable moiety were loaded either with the hydrophilic drug doxorubicin (DXR) or with the hydrophobic drug tamoxiphen (TMX) and allowed to interact with multilamellar PC-based liposomes bearing complementary recognizable groups. It has been established that, due to molecular recognition of these complementary liposomes, effective and fast transport of the drugs occurs from unilamellar to multilamellar liposomes. The transport of TMX is more effective compared to that of DXR. This behavior was observed for both PEGylated and non-PEGylated unilamellar liposomes, and it was attributed to the different sites of solubilization of the drugs in the unilamellar liposomes. PEGylation reduces the transport of both drugs since it inhibits to some extent the molecular recognition effectiveness of the complementary moieties.
带有可识别部分的单层基于磷脂酰胆碱（PC）的脂质体，要么装载亲水性药物阿霉素（DXR），要么装载疏水性药物他莫昔芬（TMX），并使其与带有互补可识别基团的多层基于PC的脂质体相互作用。已经确定，由于这些互补脂质体的分子识别作用，药物能有效且快速地从单层脂质体转运到多层脂质体。与DXR相比，TMX的转运更有效。在聚乙二醇化和非聚乙二醇化的单层脂质体中均观察到这种行为，这归因于药物在单层脂质体中的不同溶解位点。聚乙二醇化降低了两种药物的转运，因为它在一定程度上抑制了互补部分的分子识别效果。
