本發明係關於一種改進並增強生物活性劑遞送經皮膚給藥之遞送方法及組成物。該方法包含將有下列所示物之有效給予劑量:(a)藥物載劑;(b)封裝於該藥物載劑中之生物活性劑;(c)多數經共軛於該藥物載劑表面上之蛋白分解酵素分子;及(d)給藥於皮膚組織的醫藥上可接受之載體的組成物給予皮膚,據此使該生物活性劑得以依所希望劑量於一段有效時間達成遞送通過皮膚之功效者。Methods and compositions for enhancing transdermal delivery of a bioactive agent. The method contains the step of applying to a skin tissue an effective amount of a composition comprising: (a) a drug vehicle; (b) a bioactive agent encapsulated within the drug vehicle; (c) a plurality of proteolytic enzyme molecules conjugated onto the surface of the drug vehicle; and (d) a pharmaceutically acceptable carrier, for a period of time effective to deliver the bioactive agent across the skin tissue at a desired dosage.