The present invention is related to a compound conjugating a drug with a glycosaminoglycan, such as hyaluronic acid (HA), where the drug is useful for the treatment of diseases such as inflammation, auto-immune disease, allergy, infection and preferably cancer. The conjugated compound of the present invention can increase the concentration of drug at the specific site of disease by an interaction of the glycosaminoglycan used as target drug delivery carrier and the CD44 cell surface receptor, then enhancing the therapeutic efficacy and reducing the systemic side effect of the site-delivered drug.本發明係關於一種化合物,其係由一藥物與糖胺聚醣鍵結所形成,其中糖胺聚醣係以玻尿酸為例,且該藥物是用於治療疾病,例如發炎、自體免疫疾病、過敏、感染或癌症。本發明所述之經鍵結的化合物可藉由糖胺聚醣作為藥物傳遞載體而於疾病之標的位置增加藥物的濃度,並藉由CD44細胞表面受體與糖胺聚醣的相互作用以提高治療效果及減少藥物的全身性副作用。