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A pH-sensitive tumor-targeted recombinant high-density lipoprotein, preparation method and application

A high-density lipoprotein and tumor-targeting technology, applied in the field of recombinant high-density lipoprotein and its preparation, to improve anti-tumor efficacy, ensure structural stability, and improve efficiency

Active Publication Date: 2021-04-30
XUZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There is no report in this area in the prior art

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  • A pH-sensitive tumor-targeted recombinant high-density lipoprotein, preparation method and application
  • A pH-sensitive tumor-targeted recombinant high-density lipoprotein, preparation method and application
  • A pH-sensitive tumor-targeted recombinant high-density lipoprotein, preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0034]A pH-sensitive tumor-targeting recombinant high-density lipoprotein, which comprises the following components: 10 mg paclitaxel, 150 mg soybean lecithin, 150 mg bovine serum albumin, 25 mg n-butyraldehyde dicholesterol, and 25 mg linoleic acid.

[0035] The preparation method of n-butyraldehyde dicholesterol: add cholesterol and n-butyraldehyde in a molar ratio of 2.5:1 into a brown bottle, then add dichloromethane to dissolve, pass in dry hydrogen chloride gas for 20 minutes while stirring, and finally cap the bottle and continue The reaction was stirred for 6h, and the product was vacuum-dried to obtain the obtained product. The mass spectrum of the product can be seen in figure 1 , see the H NMR spectrum figure 2 ,comprehensive figure 1 The molecular weight of the compound reacted by mass spectrometry and figure 2 The characteristic chemical shift value of the acetal bond in the H NMR spectrum can prove that the synthesized product is the expected acetal substanc...

Embodiment 2

[0042] A pH-sensitive tumor-targeting recombinant high-density lipoprotein, which comprises the following components: 5 mg of paclitaxel, 150 mg of lecithin, 150 mg of bovine serum albumin, 25 mg of n-hexanal dicholesterol, and 25 mg of linoleic acid.

[0043] The preparation method of n-hexanal dicholesterol acetal: add cholesterol and n-hexanal in a molar ratio of 2.5:1 into a brown bottle, then add dichloromethane to dissolve, pass in dry hydrogen chloride gas for 20 minutes while stirring, and finally cover the bottle and continue stirring After reacting for 6h, the product was vacuum-dried to obtain.

[0044] The preparation method of the pH-sensitive tumor-targeted recombinant high-density lipoprotein is the same as that in Example 1.

Embodiment 3

[0046] A pH-sensitive tumor-targeting recombinant high-density lipoprotein, which comprises the following components: 5 mg of paclitaxel, 150 mg of soybean lecithin, 150 mg of bovine serum albumin, 25 mg of n-butyraldehyde dicholesterol, and 25 mg of linoleic acid.

[0047] The preparation method of n-butyraldehyde dicholesterol is the same as in Example 1.

[0048] Preparation method of pH-sensitive tumor-targeted recombinant high-density lipoprotein:

[0049] a) Paclitaxel, soybean lecithin, n-butyraldehyde dicholesterol, and linoleic acid are mixed and dissolved in an organic solvent (a mixed solvent with a volume ratio of methanol and methylene chloride of 8:2), and then evaporated under reduced pressure to remove the organic solvent to obtain Lipid film mixture;

[0050] b) Add 75 mg of surfactant poloxamer to 15 mL of Tris-HCL buffer at pH 8.0, mix well to obtain a hydration medium, and add the hydration medium to the lipid film mixture obtained in step a) to form a lip...

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Abstract

The invention relates to a pH-sensitive tumor-targeted recombinant high-density lipoprotein, which contains the following components in parts by weight: 1-5 parts of antitumor drugs, 15-35 parts of phospholipids, 15-60 parts of albumin, and 1-10 parts Cholesterol derivatives, 2-6 parts of linoleic acid. The pH-sensitive cholesterol derivatives in the components effectively ensure the structural stability of rHDL during blood circulation and delivery, and improve the efficiency of targeted delivery of anti-tumor drugs to tumor tissues. After rHDL is taken up by tumor cells, the pH-sensitive cholesterol derivatives The acetal bond in the substance is hydrolyzed into the original cholesterol, which satisfies the catalytic conditions of the intracellular ACAT enzyme, and realizes the rapid release of anti-tumor drugs in the tumor cells through the change of the lipoprotein structure, and effectively kills the tumor cells. A tumor-targeting carrier with great development potential solves the problems of low bioavailability and low tumor killing selectivity of anti-tumor drugs in the prior art.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pH-sensitive tumor-targeting recombinant high-density lipoprotein and a preparation method. Background technique [0002] At present, anti-tumor drugs, especially fat-soluble anti-tumor drugs, generally have problems such as low bioavailability and low tumor killing selectivity, for example, paclitaxel and doxorubicin, although they have good anti-tumor activity, their solubility in water is low (<0.03g / L), wide range of action, weak specificity, strong toxic and side effects, so its oral preparations and injections have encountered problems such as low bioavailability and low tumor killing selectivity in clinical application, so clinical treatment There is an urgent need for an effective method to improve the solubility of fat-soluble antineoplastic drugs, reduce the toxic and side effects of antineoplastic drugs, and increase the tumor killing effect of antine...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/337A61K31/704A61K47/42A61K47/24A61K47/28A61P35/00C07J9/00
CPCA61K9/1275A61K31/337A61K31/704A61K47/24A61K47/28A61K47/42A61P35/00C07J9/00
Inventor 李瑾周凯韩蒙蒙李健飞王倩倩葛志名邹佳辉
Owner XUZHOU MEDICAL UNIV
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