功能性磷脂的合成及剪切力敏感型脂质体的制备

发布时间：2018-11-16 21:48

【摘要】：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。
[Abstract]:In this study, a new phospholipid material, 1ttri-dipalmaminophospholipidine-Pad-PC-Pad, was synthesized and shear-sensitive liposomes (shear-stress sensitive liposomes,SSSL) were prepared. Firstly, the characterization of a new phospholipid material, Pad-PC-Pad, NMR and MS, showed that the synthesis was successful. Secondly, shear-sensitive liposomes were prepared by hydration dispersion method with Pad-PC-Pad as membrane material, and encapsulated with aggregation-caused quenching,. The shear stress sensitivity and release characteristics of the preparation in the narrow site were investigated by using the fluorescent dye calcium xanthocyanine (ACQ). The results showed that the particle size of liposome was 106.91 卤1.24 nm, which was ellipsoidal under transmission electron microscope. The release of the inclusions increased with the increase of ultrasonic power, which indicated that the carrier was sensitive to shear stress. In addition, the liposome was subjected to high shear stress in the narrow area and had the characteristics of rapid release. In this study, a functional phospholipid Pad-PC-Pad, was synthesized. The liposome prepared by the phospholipid has shear stress sensitivity and is expected to be used in the specific treatment of thrombus site.
【作者单位】：南昌大学药学院;中国科学院上海药物研究所;
【基金】：国家自然科学基金资助项目(81571796) 中国科学院青年创新促进会资助项目(2015229)
【分类号】：R943

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