Abstract: The present invention relates to a composition and method for therapeutic treatment of humans and other mammals. The present invention may address drug resistance problems in vivo. The therapeutic composition of the present invention comprises an encapsulation vesicle, an activation agent such as a pore forming agent on the surface of the encapsulation vesicle and an optional targeting ligand. The targeting ligand may be attached to either the activation agent or the encapsulation vesicle. The encapsulation vesicle may contain a bioactive agent that may be released to the inside of a diseased cell. The activation agent or pore forming agent is activated by an activation condition.