Polymeric micelles anchored with TAT for delivery of antibiotics across the blood–brain barrier

Polymeric micelles selfassembled from cholesterolconjugated polyethylene glycol PEG and anchored with transcriptional activator TAT peptide TATPEGbCol were fabricated for delivery of antibiotics across the blood–brain barrier BBB. Ciprofloxacin, which demonstrated a high bactericidal effect, was efficiently loaded into the micelles by a membrane dialysis method. The ciprofloxacinloaded micelles were characterized via dynamic light scattering and SEM. The micelles were spherical in nature, having an average diameter of smaller than 180 nm. Sustained release of ciprofloxacin was achieved over 6 h in phosphatebuffered saline pH 7.4 at 37°C. Confocal laser scanning microscopy reveals that the uptake of Fluorescein 5isothiocyanate FITCloaded TATPEGbCol micelles by human astrocytes was much higher than that of free FITC. Animal studies proved that these micelles crossed the BBB and entered the brain. The TATconjugated micelles may be used to deliver antibiotics across the BBB for treatment of brain infections. © 2008 Wiley Periodicals, Inc. Biopolymers Pept Sci 90: 617–623, 2008.This article was originally published online as an accepted preprint. The “Published Online” date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymerswiley.com