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Nanometer preparation of anticancer natural product (gambogic acid) and preparation method thereof

A nano-preparation and natural product technology, which is applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, drug delivery, etc., can solve the problem of limiting the use of anti-cancer drugs and the absorption and release of effective ingredients Long time, acute toxicity and side effects, etc., to achieve the effect of improving anti-tumor effect, improving bioavailability, and reducing toxic and side effects

Inactive Publication Date: 2018-10-09
SICHUAN PROVINCIAL PEOPLES HOSPITAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Based on the above physical and chemical properties, gambogic acid, as a purely natural traditional Chinese medicine anticancer drug, often has long absorption and release time and unstable release of the active ingredients in the existing clinical use, and sudden release of the active ingredients leads to acute toxic side effects However, it greatly limits its application in the preparation of anticancer drugs and its anticancer efficacy.

Method used

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  • Nanometer preparation of anticancer natural product (gambogic acid) and preparation method thereof
  • Nanometer preparation of anticancer natural product (gambogic acid) and preparation method thereof
  • Nanometer preparation of anticancer natural product (gambogic acid) and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Adopt thin film hydration method, take by weighing 20mg gambogic acid standard substance, the mPEG-PCL polymer of 200mg be placed in the round bottom flask, then completely dissolve gambogic acid standard substance and mPEG-PCL polymer in 10ml acetone. After it is completely dissolved, use a rotary evaporator to evaporate the acetone solution in the round-bottomed flask until it is completely evaporated to dryness in a water bath at 50°C, and a yellow transparent hydration film is formed at the bottom of the round-bottomed flask; stop the rotary evaporation, add 10 mL, 40 ℃ physiological saline, shake the round bottom flask quickly, then get the target product gambogic acid nano-micelle solution. The drug loading determined by HPLC method was 5.96%, and the encapsulation efficiency was 65.52%.

Embodiment 2

[0043] Adopt film hydration method, take by weighing 20mg gambogic acid standard substance, the mPEG-PCL polymer of 1g is placed in the round bottom flask, then completely dissolve gambogic acid standard substance and mPEG-PCL polymer in 20ml acetone. After it is completely dissolved, use a rotary evaporator to evaporate the acetone solution in the round bottom flask until it is completely evaporated to dryness under the condition of a water bath at 60°C, and when a yellow transparent hydration film is formed at the bottom of the round bottom flask, stop the rotary evaporation and add 15mL of physiological saline at 60°C, shake the round-bottom flask quickly to obtain the target product gambogic acid nanomicelle solution. The drug loading determined by HPLC method is 1.88%, and the encapsulation efficiency is 95.78%

Embodiment 3

[0045] Adopt thin film hydration method, take by weighing the mPEG-PCL polymer of 20mg gambogic acid standard substance, 2g and place in the round bottom flask, then completely dissolve gambogic acid standard substance and mPEG-PCL polymer in 25ml acetone. After it is completely dissolved, use a rotary evaporator to evaporate the acetone solution in the round-bottomed flask at 80°C until it is completely evaporated to dryness, and a yellow transparent hydration film is formed at the bottom of the round-bottomed flask; normal saline, shake the round-bottomed flask quickly to obtain the target product gambogic acid nano-micelle solution. The drug loading determined by HPLC method is 0.98%, and the encapsulation efficiency is 97.98%

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Abstract

The invention relates to the field of medical preparation and polymer materials, and particularly discloses a nanometer preparation of an anticancer natural product (gambogic acid). The nano preparation comprises methoxy polyethylene glycol-polycaprolactone polymer (mPEG-PCL) and gambogic acid, and is formed by encapsulating gambogic acid by methoxy polyethylene glycol-polycaprolactone in a micelle form, wherein the mass ratio of gambogic acid to methoxy polyethylene glycol-polycaprolactone is 1:(5-300). Experimental studies show that when the specific biocompatible material (mPEG-PCL) encapsulates gambogic acid, and the preferred definition of the relationship of dosage of the two is combined, the dispersion of gambogic acid in water can be effectively improved, and the bioavailability and the druggability of the nanometer preparation are enhanced; the anti-tumor effect of gambogic acid is significantly enhanced through passive targeting effect, toxic and side effects are reduced, andtreatment costs are reduced.

Description

technical field [0001] The invention relates to the fields of pharmaceutical preparations and polymer materials, in particular to a novel nano-preparation of anticancer natural drug gambogic acid and a preparation method thereof. Background technique [0002] Gambogic acid is one of the active ingredients extracted from Garcinia Cambogia. It has medicinal value such as hemostasis, anti-inflammation, detoxification, and deworming. It is also used as a diuretic abroad to treat edema and cerebral hemorrhage. Elevated blood pressure has been included in the 10th edition of the United States Pharmacopoeia. In recent years, domestic pharmacological studies have found that gambogic acid has strong anti-tumor activity in various tumors, such as leukemia, liver cancer, head and neck cancer, breast cancer, gastric cancer, pancreatic cancer, prostate cancer, cervical cancer and lung cancer, etc. , and its mechanism of action mainly includes induction of tumor cell apoptosis, inhibitio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/69A61K31/352A61P35/00A61P35/02
CPCA61K9/1075A61K31/352A61K47/6907A61P35/00A61P35/02
Inventor 蔡璐璐巩长旸童荣生王强余继英王岩
Owner SICHUAN PROVINCIAL PEOPLES HOSPITAL
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