Practical development of the lipid vesicle as surfactant assemblies having a functional molecular-recognition -toward to a cancer therapy in DDS-

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The main purpose of this work is the new preparation of the lipid vesicles, which have a function of specific targeting to a cancer cell to apply to a cancer therapy in DDS : the vesicles are mainly composed of Span80 (sorbitan monooleate) and the stability is very excellent.First, as a targeting ligand to a cancer cell as "missile device" which was immobilized to the vesicle, new alga lectin was chosen. The alga lectin was extracted and purified from a red alga, Eucheuma serra. The lectin was abbreviated as ESA (Eucheuma serra agglutinin). The ESA associates with high-mannose type carbohydrate chain specifically. The ESA-imoobilized vesicle (abbreviated as ESA-vesicle) was found to specifically combine with cancer cells, such as human colon adenocarcinoma (colo201) and not to combine to MCF10-2A and Fibroblast as a normal cell lines. The ESA had an excellent heat-stability and the inhibition of the growth of a cancer cell. Thus, ESA can be applied to both the targeting ligand and canc … More er cell or the inhibitor of cancer-cell growth. The growth inhibition was also found to induce an apoptosis. The ESA-vesicle flew smoothly in the superior artery of rabbit.The in-vivo experiments on the injection of the ESA-vesicle into rats suggested no cytotoxic effect of the vesicle on the rats because of the rat's living during 5 weeks without decrease in the weight. Moreover, in the in-vivo experiments on the injection of the ESA-vesicle into the nude mouse carrying colo201, the growth inhibition of the colo201 was aiso observed. Thus, the ESA-vesicle is expected to using for the cancer therapy in DDS.Next, some kinds of antibodies as a "missile device" as mentioned above were also immobilized on the Span80 vesicle. The specifical combines of the immunovesicles with each targeting cell were successfully confirmed the tageting experiments in vitro. The transfection of the DNA or prasmid entrapped in the immunovesicles to the targeting cells were also confirmed.Thus, the above ESA-vesicles as well as an immunovesicle were expected to be applied to either DDS or gene transfection. Less