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Trastuzumab-mediated cis-platinum targeting conjugate and preparation method thereof

A technology of trastuzumab and conjugates, which is applied in the field of biomedical technology and nanomedicine, can solve the problems of weak targeting, and achieve the effect of simple preparation process, good application prospect and good stability

Inactive Publication Date: 2015-08-26
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drugs prepared by these methods can effectively reduce the toxic and side effects and increase the circulation time of the drugs in the body, but there is still the problem of poor targeting

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0031] Preparation of methoxy-polyethylene glycol-polyglutamic acid (mPEG-PGA)

[0032] mPEG-NH 2 (5000Da, 1.00g, 0.2mmol) was dissolved with 10ml of anhydrous THF solvent, transferred to a 50ml three-neck flask, and Glu-NCA (1.08g, 4mmol) was dissolved with 5ml of anhydrous THF and placed in a constant pressure titration funnel. Under the protection of nitrogen, slowly drop into the THF solution of Glu-NCA, react at room temperature for 3d, TLC tracking (MeOH:DCM:NH 3 ·H 2 O=10:89:1; Rf=0.3). After the reaction was completed, the reaction solution was slowly poured into 150 ml of glacial ether and vigorously stirred. Freeze overnight, filter, and wash the filter cake three times with glacial ether to obtain 1.83 g of white precipitate, with a yield of 88.0%. 1 H NMR (300HMz, CDCl 3 ): δ3.6ppm (-CH 2 -O-CH 2 ), δ5.0ppm (-CH 2 -C 6 h 5 ).

[0033] Preparation of nanospheres loaded with cisplatin

[0034]Weigh 40 mg of mPEG-PGA and dissolve in 10 ml of DMF solvent, s...

example 2

[0038] Preparation of methoxy-polyethylene glycol-polyglutamic acid (mPEG-PGA)

[0039] mPEG-NH 2 (2000Da, 0.40g, 0.2mmol) was dissolved with 10ml of anhydrous THF solvent, transferred to a 50ml three-necked flask, and Glu-NCA (1.08g, 4mmol) was dissolved with 5ml of anhydrous THF and placed in a constant pressure titration funnel. Under the protection of nitrogen, slowly drop into the THF solution of Glu-NCA, react at room temperature for 3d, TLC tracking (MeOH:DCM:NH 3 ·H 2 O=10:89:1; Rf=0.3). After the reaction was completed, the reaction solution was slowly poured into 150 ml of glacial ether and vigorously stirred. Freeze overnight, filter, and wash the filter cake three times with glacial ether to obtain 1.12 g of white precipitate with a yield of 85.9%. 1 HNMR (300HMz, CDCl 3 ): δ3.6ppm (-CH 2 -O-CH 2 ), δ5.0ppm (-CH 2 -C 6 h 5 ).

[0040] Preparation of nanospheres loaded with cisplatin

[0041] Weigh 40 mg of mPEG-PGA and dissolve in 10 ml of DMF solvent, ...

example 3

[0045] Preparation of methoxy-polyethylene glycol-polyglutamic acid (mPEG-PGA)

[0046] mPEG-NH 2 (5000Da, 1.00g, 0.2mmol) was dissolved with 10ml of anhydrous THF solvent, transferred to a 50ml three-neck flask, and Glu-NCA (1.08g, 4mmol) was dissolved with 5ml of anhydrous THF and placed in a constant pressure titration funnel. Under the protection of nitrogen, slowly drop into the THF solution of Glu-NCA, react at room temperature for 3d, TLC tracking (MeOH:DCM:NH 3 ·H 2 O=10:89:1; Rf=0.3). After the reaction was completed, the reaction solution was slowly poured into 150 ml of glacial ether and vigorously stirred. Freeze overnight, filter, and wash the filter cake three times with glacial ether to obtain 1.65 g of white precipitate with a yield of 86.7%. 1 HNMR (300HMz, CDCl 3 ): δ3.6ppm (-CH 2 -O-CH 2 ), δ5.0ppm (-CH 2 -C 6 h 5 ).

[0047] Preparation of docetaxel-loaded nanospheres

[0048] Weigh 40 mg of mPEG-PGA and dissolve in 10 ml of DMF solvent, stir fo...

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Abstract

The invention relates to medicine technical field, and particularly relates to a preparation method of a trastuzumab-mediated cis-platinum targeting conjugate and application of the trastuzumab-mediated cis-platinum targeting conjugate in the preparation of a breast cancer resistant drug. Amphiphilic block copolymer methoxy polyethylene glycol-polyglutamic acid (mPEG-PGA) prepared from methoxypolyethylene glycol amine and 5-benzyl L-glutamate N-carboxyanhydrie is used as a base material for preparation of cis-platinum loading nano balls through the membrane dialysis method, and a carrier is connected with trastuzumab by carrier surface carboxyl group to prepare the trastuzumab-mediated cis-platinum targeting conjugate. The trastuzumab-mediated cis-platinum targeting conjugate can be targeted to enrich chemotherapy drugs in tumor site so as to directly kill tumor cells, reduce the side and toxic effects of traditional antitumor drugs, and trastuzumab targeting therapy of HER2 positive breast cancer patients can be implemented. The trastuzumab-mediated cis-platinum targeting conjugate can cleverly realize trastuzumab and cis-platinum combined targeted drug delivery way, and has good application prospect in treatment of breast cancer by combination of trastuzumab and chemotherapy.

Description

technical field [0001] The invention relates to medicines in the fields of biomedicine technology and nanomedicine and a preparation method thereof, in particular to the preparation and application of a trastuzumab-mediated cisplatin targeting conjugate. Background technique [0002] Breast cancer is one of the most common malignant tumors in women. Its incidence rate is increasing year by year, and the age of onset is decreasing, which seriously endangers women's physical and mental health and even their lives. The treatment of breast cancer is usually through surgery, chemotherapy, radiotherapy and other treatment methods. However, some patients have no obvious effect of these treatments, and some cancers will still recur and metastasize. Finding better treatment options is still an urgent problem to be solved. [0003] With the development of medical science, people have conducted in-depth research on the pathogenesis of malignant tumors, and the mechanism of gene carcin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K33/24A61K39/395A61P35/00
Inventor 邹志红庄四良孙柏旺
Owner SOUTHEAST UNIV
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