Preparation method and antitumor enhancement application of dual-targeting delivery chemotherapeutic drug nanosystem

A chemotherapeutic drug and dual-targeting technology, applied in the field of medicine, can solve the problems of fast metabolism in the body, short validity period, and large side effects, and achieve the effect of enhancing the enrichment ability.

Inactive Publication Date: 2016-05-04
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

5-Fluorouracil has a broad anti-tumor spectrum and is suitable for breast cancer, gastric cancer, liver cancer, etc., but the metabolism in the body is fast and the validity period is short. Like other chemotherapy drugs, when patients are directly applied with 5-fluorouracil, the side effects are relatively large

Method used

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  • Preparation method and antitumor enhancement application of dual-targeting delivery chemotherapeutic drug nanosystem
  • Preparation method and antitumor enhancement application of dual-targeting delivery chemotherapeutic drug nanosystem
  • Preparation method and antitumor enhancement application of dual-targeting delivery chemotherapeutic drug nanosystem

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1: the preparation method of targeting nanogel

[0050] 1. Dissolve 0.84g of 25kPEI into 20ml of Milli-Qwater, and adjust the pH to 7 with hydrochloric acid;

[0051] 2. Accurately weigh 0.4746g of NIPAM crystals and 13.146mg of BIS crystals into the above solution;

[0052] 3. Transfer the above mixture to a 50ml ground-necked flask, and add 10ml Milli-Qwater;

[0053] 4. Immerse the bottom of the flask into a constant temperature magnetic stirrer containing silicone oil, and heat the silicone oil to 50°C while stirring;

[0054] 5. Inject high-purity nitrogen into the system and stir for 30 minutes;

[0055] After 6.30 minutes, heat the silicone oil to 80°C, and add 250 μl of 0.01M tert-butyl hydroperoxide (TBHP) to the system;

[0056] 7. At 80°C, maintain a nitrogen atmosphere and stir for another 2 hours;

[0057] After 8.2 hours, stop N 2 , pass into O 2 , stirred overnight;

[0058] 9. Collect the prepared microgel, purify the microgel with a fl...

Embodiment 2

[0061] Example 2: Identification of Targeted Nanogel Components

[0062] 1. Freeze-dry the microgel after dialysis (25KPEI content is 60%);

[0063] 2. Take an appropriate amount of microgel powder and dissolve it in D 2 O, 1 H-NMR test microgel components; NIPAM contains amide bonds (δ, 5.0-8.0), PEI contains amines (δ, 0.5-5.0), microgels obtained from synthesis 1 In the H-NMR spectrum, it can be found that there are proton absorption peaks of amide bonds and amine proton absorption peaks of PEI. It can be seen that we have successfully grafted PEI and PNIPAM to form nanogel copolymers.

Embodiment 3

[0064] Embodiment 3: the test of target nano microgel particle size

[0065] 1. Dilute the dialyzed microgel with an appropriate amount of Mi1li-Qwater;

[0066] 2. Take 1ml of microgel solution, after confirming that no air bubbles are generated in the measurement container, add it into the sample pool, and repeat the measurement 3 times for each sample. The measurement conditions are: 170 scattering angle, 25°C.

[0067] Experimental results such as figure 2 As shown, with the increase of the PEI content in the microgel carrier, from 0% to 70%, its particle size gradually decreased from 493±55nm to 255.2±30nm, this is because with the increase of the PEI content in the carrier, the microgel The closer the crossover of the gel, the more positive charge the microgel carries gradually, which is conducive to the stability of the system and the increase of the drug loading capacity.

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Abstract

The invention relates to the technical field of medicines, and discloses a dual-targeting delivery chemotherapeutic drug nanosystem, and a preparation method and an antitumor enhancement application. The drug carrier of the dual-targeting delivery chemotherapeutic drug nanosystem adopts temperature-sensitive poly(N-isopropylacrylamide) as a core and positively charged polyethyleneimine as a shell; the loaded chemotherapeutic drug is 5-fluorouracil; and the drug carrier is connected with an anti-Her-1 antibody through maleimide-polyethylene glycol-succinimide acetate. An experiment result of the dual-targeting delivery chemotherapeutic drug nanosystem shows that the dual-targeting delivery chemotherapeutic drug nanosystem has good biocompatibility, and compared with free drugs, the dual-targeting delivery chemotherapeutic drug nanosystem has the advantages of enhancement of enrichment of drugs in tumor positions, enhancement of the antitumor effect and great reduction of the toxic and side effects of chemotherapeutic drugs through an EPR effect, temperature sensitivity and antibody multiple targeting.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to a nano system for dual-target delivery of chemotherapeutic drugs, its preparation method and its application in enhancing anti-tumor. Background technique: [0002] Conventional anti-cancer treatments aim at directly killing tumor cells, inevitably killing normal human cells and destroying the immune system, thereby causing severe systemic toxicity. The way of drug administration plays a big role in the drug efficacy. Many drugs have an optimum concentration range, that is, the ideal drug effect can be produced in this range, and the drug effect will be affected if the concentration is higher or lower. , and even produce toxic side effects. At the same time, the progress of research on the treatment of some major diseases is very slow, which has created the need to comprehensively use multiple strategies to deliver drugs to diseased tissues. As a result, some new ideas for co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/513A61K9/50A61K47/32A61K47/42A61P35/00
Inventor 李威张歌张莉孙赟蒋成陈迪赵梦鑫柯长洪
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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