Emerging Albumin-Binding Anticancer Drugs for Tumor-Targeted Drug Delivery: Current Understandings and Clinical Translation

Hanhee Cho, Seong Ik Jeon, Cheol Hee Ahn, Man Kyu Shim, Kwangmeyung Kim

Research output: Contribution to journalReview articlepeer-review

42 Citations (Scopus)


Albumin has shown remarkable promise as a natural drug carrier by improving pharmacokinetic (PK) profiles of anticancer drugs for tumor-targeted delivery. The exogenous or endogenous albumin enhances the circulatory half-lives of anticancer drugs and passively target the tumors by the enhanced permeability and retention (EPR) effect. Thus, the albumin-based drug delivery leads to a potent antitumor efficacy in various preclinical models, and several candidates have been evaluated clinically. The most successful example is Abraxane, an exogenous human serum albumin (HSA)-bound paclitaxel formulation approved by the FDA and used to treat locally advanced or metastatic tumors. However, additional clinical translation of exogenous albumin formulations has not been approved to date because of their unexpectedly low delivery efficiency, which can increase the risk of systemic toxicity. To overcome these limitations, several prodrugs binding endogenous albumin covalently have been investigated owing to distinct advantages for a safe and more effective drug delivery. In this review, we give account of the different albumin-based drug delivery systems, from laboratory investigations to clinical applications, and their potential challenges, and the outlook for clinical translation is discussed. In addition, recent advances and progress of albumin-binding drugs to move more closely to the clinical settings are outlined.

Original languageEnglish
Article number728
Issue number4
Publication statusPublished - 2022 Apr

Bibliographical note

Funding Information:
This work was supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (NRF-2019R1A2C3006283 and NRF-2021R1C1C2005460), the KUKIST Graduate School of Converging Science and Technology (Korea University & KIST) and the Intramural Research Program of KIST.

Publisher Copyright:
© 2022 by the authors. Licensee MDPI, Basel, Switzerland.


  • albumin
  • cancer-targeted therapy
  • drug delivery system
  • prodrug

ASJC Scopus subject areas

  • Pharmaceutical Science


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