Folate-Targeted Monodisperse PEG-Based Conjugates Made by Chemo-Enzymatic Methods for Cancer Diagnosis and Treatment

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 (FA2-dPEG-DOX2). A unique feature is the use of monodisperse PEG (dPEG). The modular approach with enzyme catalysis ensures exclusive γ...

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Bibliographic Details
Published in:International journal of molecular sciences 2021-10, Vol.22 (19), p.10347
Main Authors: Nagy, Krisztina S., Toth, Krisztina, Pallinger, Eva, Takacs, Angela, Kohidai, Laszlo, Jedlovszky-Hajdu, Angela, Mathe, Domokos, Kovacs, Noemi, Veres, Daniel S., Szigeti, Krisztian, Molnar, Kristof, Krisch, Eniko, Puskas, Judit E.
Format: Article
Language:English
Subjects:
Biomedical materials
Breast cancer
Catalysis
Catalysts
Cell culture
chemo-enzymatic synthesis
Conjugation
Cytotoxicity
Doxorubicin
Flow cytometry
folate-targeted cancer diagnosis
Folic acid
Food consumption
in vitro screening
In vivo methods and tests
in vivo screening
Intravenous administration
Ligands
Localization
Medical research
Morphology
multivalency
polymer conjugates
Selectivity
Water consumption
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Summary: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 (FA2-dPEG-DOX2). 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 FA2-dPEG-DOX2 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.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms221910347