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本研究拟合成新型磷脂材料1,3-二棕榈酰胺磷脂酰胆碱(1,3-dipalmaminophospholipid,Pad-PC-Pad),并制备剪切力敏感型脂质体(shear-stress sensitive liposomes,SSSL)。首先,化学合成了新型磷脂材料Pad-PC-Pad,核磁和质谱的表征结果表明合成成功;其次,以Pad-PC-Pad为膜材,采用薄膜水化分散法制备了剪切力敏感型脂质体,并包载具有聚集淬灭(aggregation-caused quenching,ACQ)特性的荧光染料钙黄绿素对制剂在狭窄部位的剪切力敏感性和释放特性进行了考察。结果表明:脂质体粒径为106.91±1.24 nm,在透射电镜下呈椭球形。脂质体随超声功率增加内含物释放增加,表明该载体具备剪切力敏感性。另外,脂质体在狭窄部位受高剪切力作用,具有快速释放特性。本研究合成了一种功能性磷脂Pad-PC-Pad,该磷脂制备的脂质体具备剪切力敏感性,有望用于血栓部位的特异性治疗。
In this study, a new type of phospholipid material, 1,3-dipalmaminophospholipid (Pad-PC-Pad), was synthesized, and shear-stress sensitive liposomes SSSL). Firstly, a new type of phospholipid material, Pad-PC-Pad, was synthesized by chemical method. The results of NMR and mass spectrometry showed that the synthesis was successful. Secondly, the shear stress sensitive lipids The plastid, which contains the fluorescent dye calcein with aggregation-caused quenching (ACQ) property, was investigated for the shear-susceptibility and release properties of the preparation at the stenosis. The results showed that the particle size of the liposome was 106.91 ± 1.24 nm, which was ellipsoidal under transmission electron microscope. Liposomes increased with increasing ultrasound power content release increased, indicating that the carrier has shear sensitivity. In addition, liposomes are subject to high shear forces at the stenotic site with rapid release properties. This study synthesized a functional phospholipid Pad-PC-Pad, liposomes prepared with the phospholipid with shear sensitivity, is expected to be used for specific treatment of thrombotic sites.