Polymeric micelles self-assembled from cholesterol-conjugated poly(ethylene glycol) (PEG) and anchored with transcriptional activator TAT peptide (TAT-PEG-b-Col) 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 ciprofloxacin-loaded 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 phosphate-buffered saline (pH 7.4) at 37 degrees C. Confocal laser scanning microscopy reveals that the uptake of Fluorescein 5-isothiocyanate (FITC)-loaded TAT-PEG-b-Col 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 TAT-conjugated micelles may be used to deliver antibiotics across the BBB for treatment of brain infections.
(c) 2008 Wiley Periodicals, Inc.