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Polyethylene glycol-gambogic acid liposome, preparation method and application thereof in treatment of malignant tumors

A technology of polyethylene glycol and methoxypolyethylene glycol, which is applied in the direction of antineoplastic drugs, pharmaceutical formulations, organic active ingredients, etc., can solve problems such as short blood circulation time, poor preparation stability, and poor antitumor activity. Achieve the effects of improving bioavailability, delaying release, and improving water solubility

Active Publication Date: 2017-07-04
SICHUAN PROVINCIAL PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to overcome the above-mentioned deficiencies such as poor antitumor activity, short blood circulation time, poor preparation stability and large toxic and side effects existing in the existing gambogic acid dosage forms, and provide a polyethylene glycol-gambogic acid lipid The liposome has excellent water solubility, can enhance the stability and anti-tumor effect of the drug, greatly reduce the side effects of the drug, and prolong the survival of tumor-bearing mice

Method used

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  • Polyethylene glycol-gambogic acid liposome, preparation method and application thereof in treatment of malignant tumors
  • Polyethylene glycol-gambogic acid liposome, preparation method and application thereof in treatment of malignant tumors
  • Polyethylene glycol-gambogic acid liposome, preparation method and application thereof in treatment of malignant tumors

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Example 1 A polyethylene glycol-gambogic acid liposome, composed of polyethylene glycol-gambogic acid conjugates, polyethylene glycol, and vitamin E in a weight ratio of 2:1:0.2:4:15 , cholesterol and egg yolk lecithin composition

[0039] First prepare polyethylene glycol-gambogic acid conjugates, including first methoxypolyethylene glycol 2000 (mPEG 2000 ) end group oxidation to synthesize mPEG 2000 -COOH; the second step makes mPEG 2000 The hydroxyl group at one end of -COOH reacts with the C-30 carboxyl group of gambogic acid under the action of EDA and DMAP to generate polyethylene glycol-gambogic acid conjugate PEG 2000 -GA spare.

[0040] Next prepare polyethylene glycol-gambogic acid liposome, comprise the following steps:

[0041] S1 Dissolve the PEG-GA, polyethylene glycol, vitamin E, cholesterol and egg yolk lecithin in the formula amount in ethanol to form an organic phase, and heat to 45°C;

[0042] S2 Inject the above-mentioned organic phase into the ...

Embodiment 2

[0047] Example 2 A polyethylene glycol-gambogic acid liposome, composed of polyethylene glycol-gambogic acid conjugates, polyethylene glycol, and vitamin E in a weight ratio of 1:2:0.2:4:10 , cholesterol and soybean phospholipid composition

[0048] First prepare polyethylene glycol-gambogic acid conjugates, including first methoxypolyethylene glycol 1000 (mPEG 1000 ) end group oxidation to synthesize mPEG 1000 -COOH; the second step makes mPEG 1000 The hydroxyl group at one end of -COOH reacts with the C-30 carboxyl group of gambogic acid under the action of EDA and DMAP to generate polyethylene glycol-gambogic acid conjugate PEG 1000- GA spare.

[0049] The preparation method of polyethylene glycol-gambogic acid liposome, comprises the following steps:

[0050] S1 will formulate the amount of GA-mPEG 1000 , polyethylene glycol, vitamin E, cholesterol and phospholipids are dissolved in ethanol to form an organic phase, and heated to 40°C;

[0051] S2 Inject the above-me...

Embodiment 3

[0054] Example 3 A polyethylene glycol-gambogic acid liposome, composed of polyethylene glycol-gambogic acid conjugates, polyethylene glycol, and vitamin E in a weight ratio of 10:0.5:0.05:1:30 , cholesterol and distearoylphosphatidylglycerol

[0055] First prepare polyethylene glycol-gambogic acid conjugates, including first methoxypolyethylene glycol 8000 (mPEG 8000 ) end group oxidation to synthesize mPEG 8000 -COOH; the second step makes mPEG 8000 The hydroxyl group at one end of -COOH reacts with the C-30 carboxyl group of gambogic acid under the action of EDA and DMAP to generate polyethylene glycol-gambogic acid conjugate PEG 8000 -GA.

[0056] Next prepare polyethylene glycol-gambogic acid liposome, comprise the following steps:

[0057] S1 will formulate the amount of PEG-GA 8000 , polyethylene glycol, vitamin E, cholesterol and distearoylphosphatidylglycerol are dissolved in ethanol to form an organic phase, and heated to 50°C;

[0058] S2 Inject the above-ment...

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Abstract

The invention discloses a polyethylene glycol-gambogic acid liposome, which is composed of a polyethylene glycol-gambogic acid conjugate, polyethylene glycol, vitamin E, cholesterol and phospholipid in a weight ratio of 1-10:0.5-2:0.05-0.2:1-4:10-30. According to the invention, an amphiphilic polymer PEG and an antitumor drug gambogic acid are connected with an ester bond into a conjugate amphipathic PEG-GA, and the PEG-GA is inserted into a liposome bimolecular layer to construct a nano targeted drug delivery system, the water solubility of the drug can be improved, also the drug stability and antitumor effect can be enhanced, drug accumulation in normal tissue can be reduced, the survival time of tumor-bearing mice is prolonged, the treatment efficacy is improved and the toxic and side effects are reduced. The invention also provides a preparation method and application of the liposome, and the liposome can be applied to treatment of lung cancer, ovarian cancer, breast cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma or brain tumors.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a polyethylene glycol-gambogic acid liposome, a preparation method and its application in treating malignant tumors. Background technique [0002] Natural products and their derivatives are playing an increasingly important role in the development of human health and medicine, Garcinia cambogia ( gamboge ): Garcinia Cambogia Garcinia hanbaryi Hook. f . Secreted dry resin. It is mainly produced in Cambodia, India, Thailand and Vietnam, and it is cultivated in Guangdong Province and Hainan Province of my country. It has long been recorded in Chinese medicine that Garcinia cambogia is cold in nature, sour, pungent, astringent, and poisonous. It has the effects of breaking blood, dispelling stagnation, detoxification, hemostasis, and killing insects. It has been used to treat scrofula, carbuncle, and boils since ancient times. Wait for the stubborn illness. Garcinia ca...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/60A61K31/352A61K47/28A61P35/00
CPCA61K9/0019A61K31/352A61K47/28
Inventor 蔡璐璐白皎皎杨艳雪钟建王岩
Owner SICHUAN PROVINCIAL PEOPLES HOSPITAL
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