This invention is about a cell-penetrating drug carrier and the application thereof. The mentioned cell-penetrating drug carrier can approach the target cell through using a proper recognizable sequence, so that the cell-penetrating drug carrier can be used to specifically delivery wanted drug to target cell. Through carrying wanted drug into the cytoplasm of the target cell by cell-penetrating peptide, the drug accumulation volume in the target cell can be efficiently increased. Preferably, through using proper bioinert polymer, the cell-penetrating peptide and the recognizable sequence can be kept from been digested before approaching the target cell.本說明書揭示一種具細胞穿膜性之藥物載體及其應用。上述具細胞穿膜性之藥物載體可藉由隨著標靶細胞來選擇適當的可辨識序列,以達到專一性傳遞欲攜帶藥物的效果;藉由穿膜胜肽將欲攜帶藥物攜入標靶細胞的細胞質,以有效增加藥物在標靶細胞內的累積量。更好的是,根據本說明書的設計,藉由選擇適當長度的生物惰性高分子,將可有效降低穿膜胜肽與可辨識序列在到達標靶細胞前被破壞,且不會干擾可辨識序列到達標靶細胞附近後必須被切斷以釋放出穿膜胜肽與藥物的預定程序。