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Probiotics folic acid targeting carrier carrying anti-cancer medicament curcumin and preparation method thereof

A technology of anticancer drug and bacterial folic acid, applied in the field of medicine, can solve the problem of low utilization of natural anticancer drug-curcumin for colon cancer and the like, and achieve the effect of improving utilization rate

Active Publication Date: 2016-08-03
SOUTH CHINA NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And by characterizing the CUR-Spore-FA carrier, the release law of curcumin in simulated gastrointestinal fluid was studied, and the results showed that the CUR-Spore-FA carrier of the present invention can not only ensure the stable release of curcumin in the intestinal tract but also There is almost no release in gastric juice, which lays a solid foundation for improving the utilization rate of natural anticancer drug-curcumin, establishing a targeted delivery system for anticancer drugs and applying it to the treatment of colon cancer, which not only solves the problem of natural anticancer drug-curcumin The problem of low utilization of the hormone reduces the toxic and side effects of the treatment of colon cancer, and makes the treatment of colon cancer targeted, which opens up a new way for the treatment of colon cancer

Method used

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  • Probiotics folic acid targeting carrier carrying anti-cancer medicament curcumin and preparation method thereof
  • Probiotics folic acid targeting carrier carrying anti-cancer medicament curcumin and preparation method thereof
  • Probiotics folic acid targeting carrier carrying anti-cancer medicament curcumin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1 Preparation of probiotic folic acid targeting carrier loaded with natural anticancer drug curcumin

[0054] The schematic diagram of CUR-Spore and CUR-Spore-FA preparation is attached figure 1 shown.

[0055] 1. Preparation of curcumin-probiotic carrier (CUR-Spore)

[0056] The curcumin probiotic carrier was constructed by the esterification reaction between the hydroxyl group on the curcumin structure and the carboxyl group of the Bacillus coagulans spore coat protein. The specific reaction is as follows:

[0057] (1) Add 0.4g of Bacillus coagulans spore powder into a 50ml beaker, add 20ml of dichloromethane, and put in an ice-salt bath to 0°C.

[0058] (2) Add 0.1 g of curcumin, 30 mg of DMAP and 30 mg of N, N-dicyclohexylcarbodiimide (DCC), oscillate evenly with ultrasound, and continue the reaction in an ice-water bath for 24 hours.

[0059] (3) Centrifuge at 10,000 rpm for 10 minutes to collect the curcumin-probiotic carrier, wash with absolute ethano...

Embodiment 2

[0065] The characterization of embodiment 2 carrier CUR-Spore-FA

[0066] 1. The standard curve of curcumin is attached figure 2 shown.

[0067] Measure the absorbance value of curcumin solution of different concentrations at 420nm by ultraviolet spectrophotometry, thus draw figure 2 the standard curve, figure 2 R 2 =0.997 reached above 0.99 level, so this standard can be used. However, the range of use of the standard curve is 0 to 5.5 μg / ml.

[0068] 2. Infrared spectrum detection

[0069] (1) Dry Spore, CUR-Spore, and CUR-Spore-FA, then put them into a mortar, add a certain amount of KBr, and grind the mixture evenly until the particle size is less than 2 μm, so as not to be affected by scattered light, then put Carry out drying treatment in the dryer, press the mixture into a transparent sheet with a pressure of about 10MPa on the hydraulic press, and measure it on the machine.

[0070] (2) Infrared spectrum (FTIR) as attached image 3 As shown, A in the figure ...

Embodiment 3

[0078] Example 3 The loading rate of curcumin loaded with probiotic spores in the carrier CUR-Spore-FA and its release in simulated gastrointestinal fluid

[0079] 1. Determination of the loading rate of curcumin loaded with probiotic spores

[0080] Ultraviolet spectrophotometer detection: According to the literature, the characteristic absorption peak of curcumin is 426nm

[0081] (1) Concrete steps of drawing the standard curve of curcumin are as follows:

[0082] ① Preparation of curcumin stock solution

[0083] Accurately weigh 1mg of curcumin and place it in a beaker, add an appropriate amount of absolute ethanol to dissolve it, transfer it to a 10mL volumetric flask, and then dilute to the mark with absolute ethanol, and use it as a curcumin stock solution for later use.

[0084]② Measure 0.1, 0.15, 0.2, 0.25, 0.3, 0.35, 0.4, 0.45, 0.5mL from the stock solution and put them in nine 10mL volumetric flasks, dilute to the mark with absolute ethanol, and shake well. Usin...

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Abstract

The invention discloses a probiotics targeting carrier carrying an anti-cancer medicament curcumin and a preparation method thereof. The preparation method includes connecting the curcumin with spore surface of bacillus coagulans by means of an esterification reaction to synthesize and obtain curcumin-probiotics carrier (CUR-Spore); and then connecting the carrier with folic acid by means of the esterification reaction to successfully prepare and obtain probiotics folic acid targeting carrier carrying curcumin (CUR-Spore-FA). The targeting medicament carrier can be used to treat colorectal carcinoma, has targeting, and can reduce the toxic and side effect of the medicament. Moreover, the bacillus coagulans can protect the curcumin in the carrier medicament, so that the carrier drug can tolerate gastric acid to get through the stomach smoothly. The carrier drug can be colonization in the intestine and germination in the intestine to release curcumin for treating colorectal carcinoma. The preparation method improves the utilization rate of curcumin, establishes a targeting conveying system of the anti-cancer medicament, can be used for treating colorectal carcinoma, and provides a novel mode of treating colorectal carcinoma.

Description

technical field [0001] The invention belongs to the technical field of medicine. More specifically, it relates to a probiotic folic acid targeting carrier loaded with anticancer drug curcumin and a preparation method thereof. Background technique [0002] Cancer has become a major threat to human health. For example, colorectal cancer (CRC) is one of the high-incidence malignant tumors in humans, and its incidence has been on the rise, and has risen to the third place in the global incidence of malignant tumors. With the change of living habits and dietary structure, people consume more lipids, and the incidence of colon cancer in my country is on the rise year by year. Colon cancer has become a very serious public health problem, seriously threatening the health and life of the people, and greatly hindering the development of my country's social economy. In-depth research on the etiology, pathogenesis and treatment methods of colon cancer is particularly important. For t...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/46A61K31/12A61K47/22A61P35/00
CPCA61K31/12A61K47/22A61K47/46
Inventor 尹亮孟展关燕清
Owner SOUTH CHINA NORMAL UNIVERSITY
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