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Fluorescently labeled Angiopep-2-conjugated-PAMAM nanoparticles to evaluate drug brain-targeted delivery performance.

Created on 02 Sep 2026

Authors

Xingyue Li, Jianxiang Wang, Yifei Wang, Fangfang Hu, Xin Yang, Jingjing Zhang, Haiyan Dong, Wen Lu

Published in

Nanomedicine (London, England). Pages 1-16. Sep 02, 2026. Epub Sep 02, 2026.

Abstract

To develop and characterize a targeted nano drug delivery system (nano-DDS), specifically fluorescently labeled Angiopep-2-conjugated PAMAM nanoparticles (FITC-APP NPs), and to evaluate its targeting efficiency and therapeutic potential both in vitro and in vivo.
Angiopep-2 was chemically conjugated to PAMAM via MAL-PEG-NHS crosslinking chemistry, followed by covalent attachment of fluorescein isothiocyanate (FITC) to yield FITC-APP NPs. Using brain microvascular endothelial cells (BMEC), glioma cells (C6 cells), and HEK-293 cells as a negative control, cell adhesion, uptake, and transport behavior were assessed. The cytotoxicity and antitumor efficacy against C6 cells were evaluated comparatively with non-targeted FITC-PAMAM NPs.
FITC-APP NPs exhibited an average hydrodynamic diameter of 32.23 ± 0.62 nm and a zeta potential of -4.36 ± 0.10 mV. Compared with non-targeted FITC-PAMAM NPs, FITC-APP NPs demonstrated significantly higher adhesion, uptake, and transport rates in BMEC and C6 cells, whereas no significant differences were observed in HEK-293 cells. Furthermore, FITC-APP NPs exerted stronger inhibitory effects on C6 cells and displayed enhanced antitumor activity in animal models relative to FITC-PAMAM NPs.
These results not only provided data support for the targeting characteristics of FITC-APP NPs, but also provided a method reference for the targeting performance assessment of brain-targeted nano-DDS.

PMID:
42683824
Bibliographic data and abstract were imported from PubMed on 02 Sep 2026.

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