Issue 6, 2022

Self-assembled dipeptide based fluorescent nanoparticles as a platform for developing cellular imaging probes and targeted drug delivery chaperones

Abstract

Self-assembled peptide-based nanostructures, comprised of naturally occurring amino acids, display excellent biocompatibility, biodegradability, flexible responsiveness, and synthetic feasibility and can be customized for various biomedical applications. However, the lack of inherent optical properties of peptide-based nanoparticles is a limitation on their use as imaging probes or drug delivery vehicles. To overcome this impediment, we generated Boc protected tyrosine–tryptophan dipeptide-based nanoparticles (DPNPs) with structure rigidification by Zn(II), which shifted the peptide's intrinsic fluorescent properties from the ultraviolet to the visible range. These DPNPs are photostable, biocompatible and have visible fluorescence signals that allow for real-time monitoring of their entry into cells. We further show that two DPNPs (PS1-Zn and PS2-Zn) can encapsulate the chemotherapeutic drug doxorubicin (Dox) and facilitate intracellular drug delivery resulting in cancer cell killing actions comparable to the unencapsulated drug. Finally, we chemically modified our DPNPs with an aptamer directed toward the epithelial cell surface marker EPCAM, which improved Dox delivery to the lung cancer epithelial cell line A549. In contrast, the aptamer conjugated DPNPs failed to deliver Dox into the cardiomyocyte cell line AC16. Theoretically, this strategy could be employed in vivo to specifically deliver Dox to cancer cells while sparing the myocardium, a major source of dose-limiting adverse events in the clinic. Our work represents an important proof-of-concept exercise demonstrating that ultra-short peptide-based fluorescent nanostructures have great promise for the development of new imaging probes and targeted drug delivery vehicles.

Graphical abstract: Self-assembled dipeptide based fluorescent nanoparticles as a platform for developing cellular imaging probes and targeted drug delivery chaperones

Supplementary files

Article information

Article type
Paper
Submitted
23 Dec. 2021
Accepted
13 Febr. 2022
First published
15 Febr. 2022
This article is Open Access
Creative Commons BY-NC license

Nanoscale Adv., 2022,4, 1694-1706

Self-assembled dipeptide based fluorescent nanoparticles as a platform for developing cellular imaging probes and targeted drug delivery chaperones

S. Sivagnanam, K. Das, M. Basak, T. Mahata, A. Stewart, B. Maity and P. Das, Nanoscale Adv., 2022, 4, 1694 DOI: 10.1039/D1NA00885D

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