0000000000414134
AUTHOR
Laura K. Müller
Evaluation of multifunctional liposomes in human blood serum by light scattering.
To overcome the limited functionality of "stealth" lipids based on linear poly(ethylene glycol) (PEG) chains, hyperbranched polyether-based lipids that bear multiple hydroxyl groups for further chemical modification may be a suitable replacement. This study focuses on the development and characterization of "stealth" liposomes modified with a novel hyperbranched polyglycerol lipid (cholesterol-PEG30-hbPG23). An emphasis was placed on the stability of these liposomes in comparison to those containing a linear PEG derivative (cholesterol-PEG44) directly in human blood serum, characterized via dynamic light scattering (DLS). Polymer lipid contents were varied between 0 and 30 mol %, resulting …
Physicochemical and Preclinical Evaluation of Spermine-Derived Surfactant Liposomes for in Vitro and in Vivo siRNA-Delivery to Liver Macrophages
Herein we report on a liposomal system for siRNA delivery consisting of cholesterol (Chol), distearoylphosphatidylcholine (DSPC), and surfactant TF (1-hydroxy-50-amino-3,4,7,10,13,16,19,22-octaoxa-37,41,45-triaza-pentacontane), a novel spermine derivative (HO-EG8-C12-spermine) which has shown improved siRNA delivery to cells in vitro and in vivo. Predominantly single-walled liposomes with reproducible sizes and moderately broad size distributions were generated with an automated extrusion device. The liposomes remained stable when prepared in the presence of siRNA at N/P ratios of 17-34. However, when mixed with human serum in equal volumes, larger aggregates in the size range of several hu…