Preparation method and application of recombinant lipoprotein modified by low-concentration monosialoteterahexosyl ganglioside
A technology of ganglioside and monosialic acid, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and drug combinations, etc., which can solve the problems of non-targeting, incomplete absorption, and retention time Short and other problems, to achieve important clinical application prospects, reduce preparation costs, and important research value
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Embodiment 1
[0026] Example 1: Preparation, characterization and in vitro drug sustained release assay of LT-GM1-rHDL
[0027] The LT-GM1-rHDL prepared in this example is modified with 0.1% (accounting for the molar percentage of total lipid) monosialotetrahexosyl ganglioside (GM1) and loaded with the anti-atherosclerotic drug lovastatin (LT) recombinant HDL.
[0028] (1) Preparation
[0029] The LT-GM1-rHDL was prepared using a thin film dispersion method. Quantitatively weigh 45mg egg yolk lecithin, 5mg stearylamine, 10mg cholesterol, 20mg cholesterol oleate, 15mg triglyceride and 5mg lovastatin (LT), add methanol / chloroform mixed solution (volume ratio 1:1) for dissolution; after dissolution, the solution was subjected to reduced-pressure rotary evaporation to remove the organic solvent; the lipid film was hydrated with pH 8.0 Tris-hydrochloric acid buffer, and 0.22 μm was used after ultrasonic homogenization Filter the above product with a sterile filter membrane to sterilize, and t...
Embodiment 2
[0037] Example 2: Different drug forms of lovastatin alleviate lipid deposition or foaming of macrophages in vitro
[0038] In this experiment, the samples were divided into the following 7 groups:
[0039] (1) Blank control group: mouse RAW264.7 macrophages not receiving stimulation or treatment;
[0040] (2) Positive control group: mouse RAW264.7 macrophages stimulated by oxidized low-density lipoprotein (OxLDL);
[0041] (3) Experimental group 1: mouse RAW264.7 macrophages stimulated by OxLDL and then treated with lovastatin capsule (LT-capsule);
[0042] (4) Experimental group 2: mouse RAW264.7 macrophages stimulated by OxLDL and then treated with lovastatin solution (LT-solution);
[0043] (5) Experimental group 3: mouse RAW264.7 macrophages stimulated by OxLDL and then treated with LT-NLC;
[0044] (6) Experimental group 4: mouse RAW264.7 macrophages stimulated by OxLDL and then treated with LT-rHDL;
[0045] (7) Experimental group 5: mouse RAW264.7 macrophages stimu...
Embodiment 3
[0048] Example 3: Blood residence time, liver uptake and atherosclerotic plaque targeting of different lovastatin drug forms
[0049] In this implementation, ApoE after high-fat feeding - / - (Apolipoprotein E gene knockout homozygous) male C57BL / 6 mice were used as atherosclerosis model mice. In this implementation, the model mice were specifically divided into 5 sample groups (6 mice in each group) according to the different forms of administration: LT solution administration group (LT-solution), LT capsule administration group (LT-capsule), LT -NLC administration group, LT-rHDL administration group, and LT-GM1-rHDL administration group; wherein, except that the LT capsule administration group (LT dose is 20mg / kg) is administered orally, the remaining sample groups are mice Tail vein injection administration (LT dose is 2mg / kg).
[0050] (1) Effects of different lovastatin (LT) drug forms on the LT blood residence time of mice
[0051] After each group of atherosclerosis mo...
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