Folate-Targeted Monodisperse PEG-Based Conjugates Made by Chemo-Enzymatic Methods for Cancer Diagnosis and Treatment
oleh: Krisztina S. Nagy, Krisztina Toth, Eva Pallinger, Angela Takacs, Laszlo Kohidai, Angela Jedlovszky-Hajdu, Domokos Mathe, Noemi Kovacs, Daniel S. Veres, Krisztian Szigeti, Kristof Molnar, Eniko Krisch, Judit E. Puskas
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2021-09-01 |
Deskripsi
This paper focuses on preliminary in vitro and in vivo testing of new bivalent folate-targeted PEGylated doxorubicin (DOX) made by modular chemo-enzymatic processes (FA<sub>2</sub>-dPEG-DOX<sub>2</sub>). A unique feature is the use of monodisperse PEG (dPEG). The modular approach with enzyme catalysis ensures exclusive γ-conjugation of folic acid, full conversion and selectivity, and no metal catalyst residues. Flow cytometry analysis showed that at 10 µM concentration, both free DOX and FA<sub>2</sub>-dPEG-DOX<sub>2</sub> would be taken up by 99.9% of triple-negative breast cancer cells in 2 h. Intratumoral injection to mice seemed to delay tumor growth more than intravenous delivery. The mouse health status, food, water consumption, and behavior remained unchanged during the observation.