doi:10.1038/nindia.2015.46 Published online 10 April 2015
Researchers have synthesized sugar-attached solid lipid nanoparticles that can ferry the anticancer drug docetaxel to tumour cells in brain. These lipid nanoparticles enhance the efficacy of docetaxel compared to commercially available formulations1.
Docetaxel cannot currently be used to treat brain tumours because it is unable to cross the blood–brain barrier and hence reach the brain. To overcome this problem, the researchers synthesized solid lipid nanoparticles, loaded them with docetaxel and then attached a sugar, aminophenyl-α-d-mannopyranoside, to them.
The scientists chose this sugar because it selectively binds to GLUT1 transporters, which carry sugars and sugar-attached particles across the blood–brain barrier. GLUT1 is highly expressed in brain tumour cells.
A drug release study using phosphate-buffered saline showed that the sugar- and drug-loaded nanoparticles released the drug more slowly than pure drug suspensions and nanoparticles loaded with only the drug. Furthermore, nanoparticles loaded with both the sugar and the drug were more toxic to tumour cells than nanoparticles loaded with only the drug, indicating that the sugar helped the nanoparticles to target brain tumours.
Brain distribution studies in tumour-bearing mice exhibited higher concentrations of sugar- and drug-loaded nanoparticles in the brain than those of nanoparticles loaded only with the drug and commercial formulations of the drug.