Cover Image

Improved pharmacokinetics and enhanced efficacy of the vancomycin derivative FU002 using a liposomal nanocarrier

Antibiotic resistance still represents a global health concern which diminishes the pool of effective antibiotics. With the vancomycin derivative FU002, we recently reported a highly potent substance active against Gram-positive bacteria with the potential to overcome vancomycin resistance. However,...

Full description

Saved in:
Bibliographic Details
Main Authors: Werner, Julia (Author) , Umstätter, Florian (Author) , Hertlein, Tobias (Author) , Beijer, Barbro (Author) , Kleist, Christian (Author) , Mühlberg, Eric (Author) , Zimmermann, Stefan (Author) , Haberkorn, Uwe (Author) , Ohlsen, Knut (Author) , Fricker, Gert (Author) , Mier, Walter (Author) , Uhl, Philipp (Author)
Format: Article (Journal)
Language:English
Published: February 2024
In: Nanomedicine. Nanotechnology, biology and medicine
Year: 2024, Volume: 56, Pages: 1-8
ISSN:1549-9642
DOI:10.1016/j.nano.2023.102731
Online Access:Verlag, kostenfrei, Volltext: https://doi.org/10.1016/j.nano.2023.102731
Verlag, kostenfrei, Volltext: https://www.sciencedirect.com/science/article/pii/S1549963423000825
Get full text
Author Notes:Julia Werner, MSc, Florian Umstätter, PhD, Tobias Hertlein, PhD, Barbro Beijer, PhD, Christian Kleist, PhD, Eric Mühlberg, MSc, Stefan Zimmermann, MD, Uwe Haberkorn, MD, Knut Ohlsen, PhD, Gert Fricker, PhD, Walter Mier, PhD, Philipp Uhl, PhD
Description
Summary:Antibiotic resistance still represents a global health concern which diminishes the pool of effective antibiotics. With the vancomycin derivative FU002, we recently reported a highly potent substance active against Gram-positive bacteria with the potential to overcome vancomycin resistance. However, the translation of its excellent antimicrobial activity into clinical efficiency could be hampered by its rapid elimination from the blood stream. To improve its pharmacokinetics, we encapsulated FU002 in PEGylated liposomes. For PEG-liposomal FU002, no relevant cytotoxicity on liver, kidney and red blood cells was observed. Studies in Wistar rats revealed a significantly prolonged blood circulation of the liposomal antibiotic. In microdilution assays it could be demonstrated that encapsulation does not diminish the antimicrobial activity against staphylococci and enterococci. Highlighting its great potency, liposomal FU002 exhibited a superior therapeutic efficacy when compared to the free form in a Galleria mellonella larvae infection model.
Item Description:Online verfügbar: 27. Dezember 2023, Artikelversion: 3. Januar 2024
Gesehen am 12.06.2024
Physical Description:Online Resource
ISSN:1549-9642
DOI:10.1016/j.nano.2023.102731

Similar Items