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摘要
To discover novel liposomes with increased stability, we set out to explore the self-assembly of nonionic surfactants bearing two asymmetric lipid chains and a polyethylene glycol unit. Utilizing glutamic acids as the scaffold, a row of amphiphilic derivatives were synthesized with different alkyl chains attached to both, the alpha- and gamma-carboxylic acids. Subsequently, the amine of the resulting glutamic acid derivatives was functionalized with polyethylene glycol composed of 4 and 20 ethylene glycol units. Utilizing the newly synthesized amphiphiles, stable and homogeneous lipid nanoparticles with an average size of about 120 nm were obtained. The critical micelle concentration, which was determined via the pyrene fluorescence assay, was found to be about 10 mu M. Subsequently, the lipid nanoparticles were loaded with the FDA approved fluorescein dye and excess dye was removed by size exclusion chromatography. The resulting lipid nanoparticles could be stored for three months at room temperature without observable deteriorations. Furthermore, preliminary results indicate that the lipid nano-particles derived from glutamic acid could be generated using human serum as the medium without noticeable differences in comparison with phosphate buffer.
- 出版日期2016-11
