This review focuses on the role of glycoprotein 60 (GP60) and secreted protein acidic and rich in cysteine (SPARC) as albumin receptors in the delivery of antitumor drugs. Albumin, derived from human or animal blood, is an ideal drug carrier due to its ability to bind to various biomolecules. GP60, expressed on vascular endothelial cells, enables albumin to cross the endothelial cell layer, while SPARC is overexpressed in many tumor cells but minimally expressed in normal tissue cells. The review details the research history, biological functions, and current research advances of GP60 and SPARC in the context of albumin-based drug delivery systems. It highlights the importance of maintaining albumin activity to maximize its interaction with GP60 and SPARC, which is crucial for effective cancer therapy. The review also discusses the challenges and future perspectives in the study of the interaction between albumin and these receptors, emphasizing the need for further research to optimize the design of albumin-based drug carriers for targeted delivery to tumors.This review focuses on the role of glycoprotein 60 (GP60) and secreted protein acidic and rich in cysteine (SPARC) as albumin receptors in the delivery of antitumor drugs. Albumin, derived from human or animal blood, is an ideal drug carrier due to its ability to bind to various biomolecules. GP60, expressed on vascular endothelial cells, enables albumin to cross the endothelial cell layer, while SPARC is overexpressed in many tumor cells but minimally expressed in normal tissue cells. The review details the research history, biological functions, and current research advances of GP60 and SPARC in the context of albumin-based drug delivery systems. It highlights the importance of maintaining albumin activity to maximize its interaction with GP60 and SPARC, which is crucial for effective cancer therapy. The review also discusses the challenges and future perspectives in the study of the interaction between albumin and these receptors, emphasizing the need for further research to optimize the design of albumin-based drug carriers for targeted delivery to tumors.