Title
A Versatile Brij-Linker for One-Step Preparation of Targeted Nanoparticles
Author
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Abstract
Background: Most frequently the functionalization of nanoparticles is hampered by time-consuming, sometimes harsh conjugation and purification procedures causing premature drug release and/or degradation. A strategy to circumvent multi-step protocols is to synthesize building blocks with different functionalities and to use mixtures thereof for nanoparticle preparation in one step. Methods: BrijS20 was converted into an amine derivative via a carbamate linkage. The Brij-amine readily reacts with pre-activated carboxyl-containing ligands such as folic acid. The structures of the building blocks were confirmed by different spectroscopic methods and their utility was assessed by one-step preparation and characterization of nanoparticles applying PLGA as a matrix polymer. Results: Nanoparticles were about 200 nm in diameter independent of the composition. Experiments with human folate expressing single cells and monolayer revealed that the nanoparticle building block Brij mediates a “stealth” effect and the Brij-amine-folate a “targeting” effect. As compared to plain nanoparticles, the stealth effect decreased the cell interaction by 13%, but the targeting effect increased the cell interaction by 45% in the monolayer. Moreover, the targeting ligand density and thus the cell association of the nanoparticles is easily fine-tuned by selection of the initial ratio of the building blocks. Conclusions: This strategy might be a first step towards the one-step preparation of nanoparticles with tailored functionalities. Relying on a non-ionic surfactant is a versatile approach as it might be extended to other hydrophobic matrix polymers and promising targeting ligands from the biotech pipeline.
Keywords
non-ionic surfactanttargeted deliverynanoparticlesfolic acidPEGylation
Object type
Language
English [eng]
Persistent identifier
phaidra.univie.ac.at/o:1973906
Appeared in
Title
Pharmaceutics
Volume
15
Issue
5
ISSN
1999-4923
Issued
2023
Publication
MDPI AG
Version type
Date issued
2023
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Rights
Rights statement
© 2023 by the authors
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