Elevated Cellular Uptake of Succinimide- and Glucose-Modified Liposomes for Blood-Brain Barrier Transfer and Glioblastoma Therapy.

ABSTRACT: The uptake of four liposomal formulations was tested with the murine endothelial cell line bEnd.3 and the human glioblastoma cell line U-87 MG. All formulations were composed of DPPC, cholesterol, 5 mol% of mPEG (2000 Da, conjugated to DSPE), and the dye DiD. Three of the formulations had an additional PEG chain (nominally 5000 Da, conjugated to DSPE) with either succinimide (NHS), glucose (PEG-bound at C-6), or 4-aminophenyl β-D-glucopyranoside (bound at C-1) as ligands at the distal end. Measuring the uptake kinetics at 1 h and 3 h for liposomal incubation concentrations of 100 µM, 500 µM, and 1000 µM, we calculated the liposomal uptake saturation S and the saturation half-time t_1/2. We show that only succinimide has an elevated uptake in bEnd.3 cells, which make

SUBMITTER: Lubitz LJ 

PROVIDER: S-EPMC11430759 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature