The present invention provides an apigenin vesiculation preparation and its preparation process. Said preparation composition includes (by wt%) 0.25%-20% of apigenin, 40%-90% of non-ionic surface active agent, 8.7-48.8% of cholesterol and 2%-20% of lyophilization protection agent. The described non-ionic surface active agent can be Span-20, Span-40, Span-60, Span-80, Tween-20, Tween-60, Tween-80, benzozir, maizir, poloxamer or their mixture. Said invention can be made into preparations of injection, nose drops, ointment and oral liquor, etc, and can be prepared by adopting ethyl alcohol injection method, film dispersion method, inversed phase evaporation method, hydration method, extrusion method, mechanical method and pH gradient method.