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PH-sensitive tumor targeted recombinant high-density lipoprotein as well as preparation method and application thereof

A high-density lipoprotein, tumor-targeting technology, applied in the field of recombinant high-density lipoprotein and its preparation, to achieve the effect of improving anti-tumor efficacy, improving efficacy, and delivering high specificity

Active Publication Date: 2019-04-05
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

Method used

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  • PH-sensitive tumor targeted recombinant high-density lipoprotein as well as preparation method and application thereof
  • PH-sensitive tumor targeted recombinant high-density lipoprotein as well as preparation method and application thereof
  • PH-sensitive tumor targeted recombinant high-density lipoprotein as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
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 is prepared from the following ingredients in parts by weight: 1 to 5 parts of antitumor medicine, 15to 35 parts of phospholipid, 15 to 60 parts of albumin, 1 to 10 parts of cholesterol derivatives and 2 to 6 parts of linoleic acid. The pH-sensitive cholesterol derivatives in the ingredients effectively ensure the structure stability of rHDL in the blood circulation conveying process; the targeted conveying efficiency of the antitumor medicine to the tumor tissues is improved; after the rHDL istaken by tumor cells; acetal bonds in the pH-sensitive cholesterol derivatives are hydrolyzed into the original cholesterol; the catalysis condition of intracellular ACAT enzyme is met; the fast release of the antitumor medicine in the tumor cells is realized through the lipoprotein structure change; the tumor cells are effectively killed. The lipoprotein belongs to a tumor targeted carrier with huge development potential; the problems of low bioavailability and low tumor killing selectivity of the antitumor medicine in the prior art are solved.

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 Applications(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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