Investigation of glucose-modified liposomes using polyethylene glycols with different chain lengths as the linkers for brain targeting

• DOI: 10.2147/ijn.s23771
• Publication Date: 2012-01-06T05:23:49Z
• Authors: Fulan Xie; Fulan Xie; Qin; Yuan; Tang; Zhang; Fan; Chen; Hai; Yao; Li; Qin He
• Keywords: Biodistribution; Dispersity; Ex vivo

Background: An intimidating challenge to transporting drugs into the brain parenchyma is presence of blood–brain barrier (BBB). Glucose an essential nutritional substance for function sustenance, which cannot be synthesized by brain. Its transport primarily depends on glucose transporters capillary endothelial cells. In this paper, brain-targeted properties glucose-modified liposomes using polyethylene glycols with different chain lengths as linkers were compared and evaluated establish optimized drug-delivery system. Methods: Coumarin 6-loaded (GLU200-LIP, GLU400-LIP, GLU1000-LIP, GLU2000-LIP) composed phospholipids glucose-derived cholesterols prepared thin-film dispersion-ultrasound method. The BBB model in vitro was developed evaluate transendothelial ability crossing BBB. biodistribution mice brains identified vivo ex nearinfrared fluorescence imaging confocal laser scanning microscopy further analyzed quantitatively high-performance liquid chromatography. Results: Glucose-derived identified, coumarin successfully. particle sizes four types around or smaller than 100 nm a polydispersity index less 0.300. GLU2000-LIP achieved higher cumulative cleared volumes after 6 hours GLU200-LIP ( P < 0.05) significantly that conventional liposome 0.001). qualitative quantitative results showed accumulation GLU1000-LIP highest among all groups 0.01 versus LIP). Conclusion: data indicated possess potential targeting, promising system, exhibited strongest delivery capacity. Keywords: glucose, glycols, liposome, BBB,