合成了复合脂质N,N-二-十六烷基-N^α-6-(3-三乙氧硅烷基)丙基二甲胺基己酰基-L-丙氨酰胺(1),其结构经薄层色谱(TLC)、^1 H核磁共振(NMR)及元素分析表征得以证实。将该脂质分散到水溶液中并进行超声,其头部将水解进而缩合形成表面具有陶瓷或硅覆盖的脂质体,因此将其命名为Cerasome。用十六烷基三甲基溴化铵(CTAB)作为添加的表面活性剂,采用荧光分光光度计通过测定脂质体的光散射强度,对Cerasome及作为对照的合成肽脂N,N-二-十六烷基-N^α-6-三甲胺基己酰基-L-丙氨酰胺(2)和磷脂酰胆碱(3)脂质体的稳定性进行了评价,结果Cerasome表现出了异常高的稳定性。
An organic - inorganic hybrid lipid N, N - dihexadecyl - N^α - [ 6 - [ (3 - triethoxysilyl) propyldi -methylammonio ] hexanoyl I alaninamide bromide was synthesized. The compound was characterized by thin layer chromatography,^1 HNMR spectra and elemental analysis. The lipid has a (triethoxysilyl)propyl group as an inorganic precursor on the quarternized ammonium nitrogen. Upon sonication of the lipid dispersed in aqueous HEPES buffer, it self- assembles with concomitant hydrolysis of the inorganic precursor moiety followed by condensation to give partially ceramic - or silica -coated liposome (Cerasome). Morphological stability of the Cerasome was evaluated by light scattering intensity employing a fluorescence spectrophotometer with the addition of the surfactant CTAB. For comparison, the morphological stability of liposomes derived from a synthetic peptide lipid N, N - dihexadecyl - N^α - [ 6 - ( trimethylam- monio) hexanoyl ] alanin - amide bromide (2) and a phospholipid dimyristoylphosphatidylcholine (3) were examined under the similar sonication conditions. The results indicate that the Cerasome is highly stable as compared to the conventional lioosornes.