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Copolymer for tumor radioactivity diagnosis and treatment and preparation method and application thereof

A copolymer, radioactive technology, used in the field of medicine

Inactive Publication Date: 2018-05-08
北京思如诺科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a variety of nano drug delivery systems widely studied, such as micelles, liposomes, etc., have a certain degree of enrichment in normal tissues and organs, which makes the application of these nano system radiotherapy drugs have potential risks.

Method used

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  • Copolymer for tumor radioactivity diagnosis and treatment and preparation method and application thereof
  • Copolymer for tumor radioactivity diagnosis and treatment and preparation method and application thereof
  • Copolymer for tumor radioactivity diagnosis and treatment and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] A block copolymer for radiological diagnosis and treatment of tumors, which includes a first block monomer M1 and a monomer M2 and a second block monomer M3, monomer M4 and monomer M5, the block copolymer generally The formula is shown in formula II;

[0068]

[0069] In the above general formula II, wherein, R 1 = R 2 = Equal pH-responsive groups, the dotted circle is the connection with the copolymer, R 3 =OH, cyclic RGD peptide, folic acid, aptamer or antibody, such as EGFR antibody;

[0070] The molecular weight distribution index d<1.3 of the block copolymer in the general formula I; the total number average molecular weight of the block copolymer is 10000-100000, preferably 40000-100000, more preferably 60000-98000, more preferably 70000- 95000, most preferably 80000-90000.

[0071] m is an integer of 10-70, preferably an integer of 15-65, more preferably an integer of 15-60, more preferably an integer of 20-50, most preferably an integer of 20-30;

[...

Embodiment 2

[0079] A random copolymer for tumor radiation diagnosis and treatment, which includes monomer M1 and monomer M2 and the second block monomer M3, monomer M4 and monomer M5, the general formula of the random copolymer is as formula III shown;

[0080]

[0081] In the above general formula III, wherein, R 1 = R 2 = Equal pH-responsive groups, the dotted circle is the connection with the copolymer, R 3 =OH, cyclic RGD peptide, folic acid, aptamer or antibody, such as EGFR antibody;

[0082] The molecular weight distribution index d<1.3 of the block copolymer in the general formula I; the total number average molecular weight of the block copolymer is 10000-100000, preferably 40000-100000, more preferably 60000-98000, more preferably 70000- 95000, most preferably 80000-90000.

[0083] m is an integer of 10-70, preferably an integer of 15-65, more preferably an integer of 15-60, more preferably an integer of 20-50, most preferably an integer of 20-30;

[0084] n is an in...

Embodiment 3

[0089] S1: Synthesis of M1 and M2 monomers

[0090] (1) The synthesis process of M1

[0091]

[0092] The synthesis of M1 containing tyrosine is divided into two steps. First, 5.45 g of tyrosine is refluxed overnight at 60° C. in a mixed solution of 100 ml of methanol and 4 ml of thionyl chloride. After the reaction was completed, the solvent was selectively removed, and the obtained product was washed twice with ether to obtain L-tyrosine methyl ester hydrochloride, and the yield of this step was 97%.

[0093] Suspend 2.31g of the prepared tyrosine methyl ester hydrochloride in 100ml of dichloromethane, then add 2.02g of triethylamine and stir in an ice-water bath for 1 hour, slowly add 1.43g of methyl Acryloyl chloride, after the dropwise addition, the temperature was raised to room temperature and the reaction was continued for 24 hours. After the reaction is completed, wash with 0.1M dilute hydrochloric acid and 0.1M sodium bicarbonate solution for several times, and ...

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Abstract

The invention relates to a copolymer for tumor radioactivity diagnosis and treatment and a preparation method and application thereof. The copolymer is composed of a monomer M1, a monomer M2, a monomer M3, a monomer M4 and a monomer M5 as shown in a general formula I. The copolymer includes block copolymers and random copolymers. The preparation method comprises the following steps: preparing a hetero-functionalized initiator for polymerizing and connecting each monomer, and using the hetero-functionalized initiator for polymerization to obtain the copolymer. The copolymer is mainly used for loading radioactive isotopes for diagnosis and treatment of tumors. The copolymer is used for loading the radioactive isotopes and further applied to early diagnosis of the tumors, especially for metastatic tumors, and subsequent radiotherapy in vivo. By means of preparation of a polymer system with long cycle time and very low normal tissue uptake, effective enrichment of the block copolymer within the tumors can be achieved, and the loaded radioactive isotopes of different types are combined to achieve a series of biological functions from diagnosis to treatment. The formula is shown in the description.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to a copolymer used for tumor radiation diagnosis and treatment and its preparation method and application. treat. Background technique [0002] Tumor has always been a major disease that threatens human health. Traditional treatment methods have high mortality, low cure rate and poor prognosis. The recognized method to reduce cancer mortality is early detection, early treatment, detection of cancer cells before they spread, and effective treatment. At present, the main diagnostic techniques for various malignant tumors can only detect tumors larger than 1 cm in size, but are powerless for smaller tumors, such as magnetic resonance imaging (MRI) [Biomaterials, 2011; 32:5167-5176], single photon emission Computed Tomography (SPECT), Computed Tomography (CT) and Positron Emission Tomography (PET). Medical contrast agents can improve the detection sensitivity and spatial resolution o...

Claims

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Application Information

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IPC IPC(8): C08F220/58C08F220/34C08F220/60A61K49/04A61K51/06A61P35/00A61P35/04A61K101/02
CPCA61K49/04A61K51/065C08F220/58C08F2438/01C08F2438/02C08F2438/03C08F220/34C08F220/603
Inventor 喻青松甘志华张佳婧沈毅
Owner 北京思如诺科技有限公司
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