Phenylboronic Acid-conjugated Exosomes for Enhanced Anticancer Therapeutic Effect by Increasing Doxorubicin Loading Efficiency


Anticancer drugs, including doxorubicin (DOX), have been widely used for cancer treatment, but these chemotherapeutic drugs have some issues to address because of their associated side effects, such as cytotoxicity. Various synthetic delivery vehicles for anticancer drugs have been developed to encapsulate and transfer them to cancer cells. However, these delivery vehicles also have high cytotoxicity and immunogenicity. Recently, exosomes have been highlighted as candidates for anticancer drug delivery vehicles with fewer side effects. Exosomes are nanosized particles that are produced from cells, and high concentrations of exosomes are already present in the human body. To develop exosome-based anticancer therapeutics, high drug concentrations should be loaded into exosomes. In this context, phenylboronic acid (PBA) was introduced and chemically conjugated to the exosome surface to load DOX to exosomes. Consequently, a high amount of DOX was efficiently loaded onto the PBA-conjugated exosomes. The DOX-loaded PBA-conjugated exosomes were applied to MDA-MB-231 breast cancer cells and showed enhanced cancer cell cytotoxicity compared to free DOX and DOX-loaded non-conjugated exosomes. Therefore, using PBA-conjugated exosomes for delivering DOX to cancer cells can be a promising strategy for effectively killing cancer cells because a high amount of DOX can be loaded and delivered.

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This work was supported by the Incheon National University Research Grant in 2017.

The authors declare no conflict of interest.

Neither ethical approval nor informed consent was required for this study.

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Correspondence to Won Jong Rhee.

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Kim, H., Kang, S.J. & Rhee, W.J. Phenylboronic Acid-conjugated Exosomes for Enhanced Anticancer Therapeutic Effect by Increasing Doxorubicin Loading Efficiency. Biotechnol Bioproc E 26, 78–85 (2021).

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  • doxorubicin
  • anticancer drug
  • delivery vehicles
  • exosome
  • phenylboronic acid