PURPOSE: A conjugate containing polyethyleneimine and bile acid is provided to ensure high transport efficiency and to transport nucleic acid drugs. CONSTITUTION: A conjugate containing polyethyleneimine and bile acid is conjugated by reaction of carboxy group of bile acid and amine group of polyethyleneidmine. The bile acid is cholic acid, 5 beta-cholanic acid, chenodeoxycholic acid, glycoholic acid, taurocholic acid, deoxycholic acid, lithocholic acid, or 7-oxo-lithochoilc acid. The conjugated contain macromolecule or hydrophobic drugs. The macromolecule is plasmid DNA, siRNA, or antisense oligonucleotide. The hydrophobic drug is doxorubicin, adriamycin, cisplatin, paclitaxel, taxol, docetaxel, or daunomycin.본 발명은, 거대분자를 효율적으로 세포내로 전달할 수 있는, 폴리에틸렌이민 및 담즙산으로 구성된 회합체에 있어서, 상기 담즙산의 카르복시기와 폴리에틸렌이민의 아민기의 반응에 의하여 결합된 회합체에 관한 것이다.