PURPOSE: A nanoparticle containing a low molecular weight amphiphilic hyaluronic acid composite is provided to show superior water solubility compared with an existing drug delivery system and to encapsulate high volume drugs with high efficiency. CONSTITUTION: A low molecular weight hyaluronic acid-5-beta cholanic acid composite is an amphiphilic composite in which 5-beta-cholanic acid is conjugated to hyaluronic acid with a molecular weight of 5-20 kDa. The composite forms self-aggregates in water. Nanoparticles are formed by encapsulating a hydrophobic drug in the composite. A method for preparing the nanoparticles comprises the steps of: synthesizing 5-beta cholanic acid with a cholanic acid structure using aminoethyl cholanoamide; dissolving the hyaluronic acid with a molecular weight of 5-20 kDa in an aqueous solvent to prepare a hyaluronic acid solution; dissolving aminoethyl cholanoamide in an organic solvent to prepare a cholanoamide solution; adding the cholanoamide solution to the hyaluronic acid solution and preparing a reactant solution; depositing the hyaluronic acid-5-beta cholanic acid composite from the reactant solution; and encapsulating a drug in the hyaluronic acid-5-beta cholanic acid.본 발명은 5 내지 20 KDa의 저분자량 히알루론산에 소수성 담즙산이 결합되어 수중에서 자기 집합체(self-aggregation)를 형성하는 히알루론산-담즙산 복합체, 상기 복합체 내부에 소수성 약물이 봉입된 나노입자, 그 나노입자를 포함하는 주사제, 및 그 나노입자의 제조방법을 제공한다.