A kind of preparation method of scutellarin aglycone liposome
A technology of scutellarin aglycone lipid and scutellarin aglycone, which is applied in liposome delivery, medical preparations containing non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of scutellarin aglycone High protein binding rate, influence of scutellarin aglycon stability, poor stability of scutellarin aglycone, etc., to achieve good storage stability, increase drug loading, and increase drug concentration gradient
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[0047] One, the preparation method of scutellarin aglycone liposome preparation
[0048] The preparation method of the scutellarin aglycone liposome preparation of the present invention comprises:
[0049] (1) prepare inner aqueous phase and outer aqueous phase and all contain the blank liposome of acetate aqueous solution;
[0050] (2) preparing blank liposomes whose inner water phase contains acetate aqueous solution and whose outer water phase contains physiological isotonic solution;
[0051](3) Mix the blank liposome obtained in step (2) with the scutellarin double salt solution, incubate, remove free scutellarin aglycone, and obtain a scutellarin aglycone liposome preparation.
[0052] The acetate may be calcium acetate.
[0053] The concentration of acetate in the acetate aqueous solution is greater than or equal to 150mM. The concentration of acetate in the acetate aqueous solution is greater than or equal to 300mM. The concentration of acetate in the acetate aqueo...
Embodiment 1
[0107] Preparation and characterization of embodiment 1 scutellarin aglycon double salt
[0108] 1. Preparation of scutellarin aglycon double salt
[0109] Add scutellarin aglycon and basic compound into acetonitrile according to a certain molar ratio, and stir overnight at room temperature. Centrifuge to remove acetonitrile, and wash with acetonitrile three times repeatedly, collect the obtained solid, weigh it, and determine its solubility. The results are shown in Table 1. After scutellarin aglycon and arginine form a double salt, the solubility of scutellarin aglycon is significantly improved, and the solubility improvement effect is better than that of metformin and lysine on scutellarin aglycon.
[0110] Table 1 Preparation and solubility of scutellarin aglycon double salt (mg / ml)
[0111]
[0112] 2. Characterization of scutellarin aglycon double salt
[0113] 1. Differential thermal scanning method DSC
[0114] Instrument model: DSC 204F1 from Netzsch, Germany ...
Embodiment 2
[0141] Example 2 Using scutellarin aglycone double salt solution as the external water phase and calcium acetate solutions of different concentrations as the internal water phase to prepare scutellarin aglycone liposomes with high drug loading
[0142] 1. Hydrogenated soy lecithin (HSPC) was purchased from NOF Corporation, and pegylated phospholipids: distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG2000) and cholesterol (Cholesterol) were purchased from the United States Avanti Polar Lipids; scutellarin aglycone was purchased from Nanjing Jingzhu Biotechnology Co., Ltd.; calcium acetate was purchased from Sinopharm Chemical Reagent Co., Ltd.
[0143] 2. Preparation of scutellarin aglycon liposomes
[0144] (1) Accurately weigh hydrogenated soybean lecithin (HSPC, molecular weight 783.8), cholesterol (CHOL, molecular weight 386.7) and distearoylphosphatidylethanolamine-polyethylene glycol 2000 according to the mass ratio of 3:1:1, and add an appropriate amo...
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Abstract
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