Anti-tumor nano-drug

A technology of nano-drugs and nano-drug carriers, which is applied in the direction of anti-tumor drugs, drug combinations, drug delivery, etc. It can solve the problems of proportional entry into cells, difficult to achieve, and poor curative effect, so as to improve curative effect, avoid large toxic and side effects, and not easy to remove Effect

Active Publication Date: 2018-09-21
成都登隆生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the small molecule LA has both hydrophilic and lipophilic properties, it can reach any part of the body after entering the body and is easily cleared quickly, resulting in a large dosage and poor curative effect.
Combination drugs can improve the therapeutic effect of LA, but when combined with other small molecule drugs, various drugs cannot enter the cells in a predetermined ratio, and it is difficult to achieve the effect of "1+1 greater than 2"

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Preparation of lipoic acid polymers.

[0060] Lipoic acid polymers can exist in the form of lipoic acid micelles, lipoic acid vesicles and lipoic acid aggregates, such as figure 1 Shown.

[0061] 1. Preparation of lipoic acid micelles (Cross-linked lipoic acid micelles, c-LAMs):

[0062] Add 100 mg of lipoic acid (LA) to 50 ml of deionized water, add 1 M NaOH aqueous solution dropwise with stirring until the lipoic acid is completely dissolved, then drop 1 M HCl solution until the solution is neutral, and finally freeze the solution. A pale yellow sodium lipoic acid powder was obtained. Weigh 41.2 mg (0.2 mol) of sodium lipoic acid, dissolve it in 1 ml of deionized water, and prepare nanoparticles with a size of about 15 nm after ultrasound. The nanoparticles obtained above were subjected to 365 nm ultraviolet light to initiate self-crosslinking of lipoic acid disulfide bonds, reacted for 2.5 h, and after dialysis for 48 h, cross-linked lipoic acid micelles (Cross-linked lip...

Embodiment 2

[0071] Study on the anti-tumor mechanism of lipoic acid polymer.

[0072] Select cross-linked lipoic acid micelles (c-LAMs) as an example to study the anti-tumor activity mechanism of lipoic acid polymers.

[0073] 1. Cytotoxicity assessment:

[0074] Select human colon cancer cells (SW480) in the active logarithmic growth phase, inoculate them in 96-well plates, culture for 24 hours, then add different concentrations of LA and c-LAMs to them, set different concentration gradients, and set each concentration setting 5 parallel samples and a control group. After culturing for 48 hours, remove the medium, add 100 μl of medium containing 10% (v / v) MTT and continue incubating for 2 hours, then aspirate the old medium, and then add 150 μl of DMSO to each well, and Oscillate on a shaker for 2 minutes, and finally measure the absorbance at 490 nm with a microplate reader to calculate the cell viability. The result is as follows image 3 shown in a. The experimental results found that c-L...

Embodiment 3

[0084] Evaluation of lipoic acid polymer and LA anti-tumor activity.

[0085] Choose lipoic acid micelles (c-LAMs) as an example to evaluate the anti-tumor activity of lipoic acid polymers and LA.

[0086] Human hepatocellular carcinoma cells (HepG2) in the active logarithmic growth phase were selected and seeded in 96-well plates. After 24 hours of culture, c-LAMs and LA were added. Different concentration gradients are set for the two materials, 5 parallel samples are set for each concentration, and a control group is set. After 72 hours of incubation, aspirate the old medium, add 100 μl of medium containing 10% (v / v) MTT to each well, incubate for 2 hours, aspirate the old medium, add 150 μl of DMSO to each well, and shake After oscillating on the device for 2 minutes, measure the absorbance at 490 nm with a microplate reader to calculate the cell viability. The experimental results are as follows Figure 4 As shown, c-LAMs has better anti-tumor activity than LA. The reason may...

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Abstract

The invention discloses an anti-tumor nano-drug. The anti-tumor active ingredient of the nano-drug exists mainly in the form of a lipoic acid polymer. The invention further discloses a preparation method and application of the nano-drug. The anti-tumor nano-drug solves the problem of large toxic and side effects of the traditional chemotherapeutic drug. Meanwhile, the anti-tumor active ingredientis also used in combination with other substances having the anti-tumor activity, and enters the cell at the predetermined ratio, the synergistic anti-tumor effect that one plus one is more than 2 isachieved, and the anti-tumor nano-drug has a broad application prospect.

Description

Technical field [0001] The invention belongs to the field of biological materials, and specifically relates to an anti-tumor nanometer medicine. technical background [0002] Cancer is a common and multiple major disease that seriously endangers human health, and its mortality rate accounts for the second place in the overall mortality rate of human diseases. Chemotherapy is an important method of cancer treatment. However, traditional chemotherapy drugs can easily cause toxic side effects such as liver and kidney function damage, bone marrow suppression, and reduced human immunity. Therefore, new chemotherapeutic drugs with anti-tumor activity but non-toxic or low-toxicity to normal tissues have been developed It can well solve the problems faced by traditional chemotherapy drugs. [0003] ( R )-(+)-Lipoic acid [( R )-(+)-Lipoic Acid, referred to as LA] is a type of B vitamins synthesized by lipoic acid synthase in the mitochondria. It has the functions of stabilizing blood sugar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/385A61K31/795A61K31/4745A61K31/473A61K31/704A61K31/7068A61K31/353A61K31/05A61K31/12A61K31/122A61K45/06A61P35/00
CPCA61K45/06A61P35/00A61K31/05A61K31/12A61K31/122A61K31/353A61K31/385A61K31/473A61K31/4745A61K31/704A61K31/7068A61K31/795A61K2300/00A61K9/1271A61K9/1075A61K31/01A61K31/352A61K31/17A61K47/59A61K47/6935A61K9/127A61K9/14
Inventor 张仕勇廖春燕陈英代鑫
Owner 成都登隆生物医药有限公司
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