Size-Dependency of the Surface Ligand Density of Liposomes Prepared by Post-insertion

作者：Lee Shang Hsuan; Sato Yusuke; Hyodo Mamoru; Harashima Hideyoshi^*

来源：Biological & Pharmaceutical Bulletin, 2017, 40(7): 1002-1009.

DOI：10.1248/bpb.b16-00990

• incorporation ratio
• surface ligand density
• active targeting
• liposome
• smaller size
• post-insertion method

In the active targeting of a drug delivery system (DDS), the density of the ligand on the functionalized liposome determines its affinity for binding to the target. To evaluate these densities on the surface of different sized liposomes, 4 liposomes with various diameters (188, 137, 70, 40 nm) were prepared and their surfaces were modified with fluorescently labeled ligand lipid conjugates by the post-insertion method. Each liposomal mixture was fractionated into a series of fractions using size exclusion chromatography (SEC), and the resulting liposome fractions were precisely analyzed and the surface ligand densities calculated. The data collected using this methodology indicate that the density of the ligand on a particle is greatly dependent on the size of the liposome. This, in turn, indicates that smaller lip osomes (75-40nm) tend to possess higher densities. For developing active targeting systems, size and the density of the ligands are two important and independent factors that can affect the efficiency of a system as it relates to medical use.

• 出版日期2017-7