The invention belongs to the field of biological medicine and particularly relates to a composition containing a quaternary ammonium salt compound and siRNA and a preparing method thereof. The composition contains a siRNA sequence and the quaternary ammonium salt compound or lipid with the function of the quaternary ammonium salt compound and can also contain phopholipid, cholesterol and lipid-polyethylene glycol. The composition containing the quaternary ammonium salt compound and siRNA can improve the pharmacokinetics characteristic of siRNA treatment, change bio-distribution, intracellular intake, targeting and transfection efficiency, and reduce adverse reaction.