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Polypeptide, targeted drug carrier, preparation method of targeted drug carrier, pharmaceutical composition, and preparation method of pharmaceutical composition

A drug and carrier technology, which is applied in the direction of drug combination, pharmaceutical formula, and non-active ingredients of polymer compounds, etc., can solve the problems of low tumor targeting efficiency and low penetration rate of tumor sites, etc., and achieve high-efficiency targeting and strong tumor penetration effect of ability

Inactive Publication Date: 2014-07-23
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the shortcomings of low tumor targeting efficiency and low penetration rate in tumor sites of existing targeting molecules, and provide a polypeptide with high targeting and penetration, as well as a targeting drug carrier and Its preparation method, a kind of pharmaceutical composition and its preparation method

Method used

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  • Polypeptide, targeted drug carrier, preparation method of targeted drug carrier, pharmaceutical composition, and preparation method of pharmaceutical composition
  • Polypeptide, targeted drug carrier, preparation method of targeted drug carrier, pharmaceutical composition, and preparation method of pharmaceutical composition
  • Polypeptide, targeted drug carrier, preparation method of targeted drug carrier, pharmaceutical composition, and preparation method of pharmaceutical composition

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preparation example Construction

[0033] In a fourth aspect, the present invention provides a method for preparing a pharmaceutical composition, wherein the method comprises:

[0034] (1) In an organic solvent, the hydrophobic drug is mixed with the substance containing the targeted drug carrier provided by the present invention, and then dried to remove the organic solvent to obtain a dried material;

[0035] (2) Contacting the dried material with a buffer solution.

[0036] According to the present invention, in step (1), the content of the targeted drug carrier in the substance containing the targeted drug carrier provided by the present invention can vary widely, for example, it can be 20-100% by weight. Wherein, the substances in the substances other than the targeted drug carrier of the present invention can be, for example, common drug carriers, that is, drug carriers not connected with maleamide groups, for example, distearoylphosphatidylethanolamine-polyethylene Diol 2000 (DSPE-PEG 2000 ).

[0037]...

Embodiment 1

[0050] This example is used to illustrate the polypeptide, targeted drug carrier, pharmaceutical composition and preparation method thereof provided by the present invention

[0051] (1) Weigh 3 mg of peptide and 15 mg of DSPE-PEG respectively 2000 -MAL (the molar ratio of the polypeptide to the maleamide group in the drug carrier is 1:1) and dissolved in 2 mL of 50 mM hydroxyethylpiperazineethanesulfonic acid (HEPES) buffer (pH 6.5 ) at 30°C for 48 hours, the solution after the contact was dialyzed in a dialysis bag with a molecular weight of 2000 to remove unlinked polypeptides, and after the dialysis was completed, it was freeze-dried to obtain the drug containing the targeting drug carrier of the present invention dry powder.

[0052] (2) Put 2mg of the dry powder containing the targeted drug carrier prepared in step (1) and 8mg of the common drug carrier DSPE-PEG in an eggplant-shaped bottle 2000 and 2 mg of hydrophobic doxorubicin were dissolved in 4 mL of a mixed solu...

Embodiment 2

[0055] This example is used to illustrate the polypeptide, targeted drug carrier, pharmaceutical composition and preparation method thereof provided by the present invention

[0056] (1) Weigh 15 mg of peptide and 15 mg of DSPE-PEG respectively 2000 -MAL (the molar ratio of the polypeptide to the maleamide group in the drug carrier is 5:1) and dissolved in 3 mL of 40 mM hydroxyethylpiperazineethanesulfonic acid (HEPES) buffer (pH 6.0 ) at 20°C for 60 hours, the solution after the contact is dialyzed in a dialysis membrane with a molecular weight of 2000 to remove unlinked polypeptides, and after the dialysis is completed, it is freeze-dried to obtain the target drug carrier of the present invention dry powder.

[0057] (2) Dissolve 10 mg of the dry powder containing targeted drug carrier prepared in step (1) and 1 mg of docetaxel in 3 mL of a 2:1 mixed solution of chloroform and methanol in an eggplant-shaped bottle, and Referring to the method disclosed in Pharmaceutics (Pe...

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Abstract

The invention discloses a polypeptide, which contains an amino acid sequence represented by the SEQ ID No.1. The invention also discloses a targeted drug carrier and a preparation method thereof. The preparation method comprises the following step: contacting the polypeptide provided by the invention with a drug carrier containing a group represented by the formula (1) so as to form a covalent linkage, which is represented by the formula (2), between the polypeptide and the drug carrier. The invention also discloses a pharmaceutical composition and a preparation method thereof. The preparation method comprises the following steps: (1) mixing a hydrophobic drug with a substance containing the targeted drug carrier mentioned above in an organic solvent, drying to remove the organic solvent so as to obtain a dried material; (2) contacting the dried material with a buffer solution. The polypeptide, targeted drug carrier, and pharmaceutical composition all have a high efficient targeting property and a very strong tumor penetrating performance.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a polypeptide, a targeting drug carrier and a preparation method thereof, a pharmaceutical composition and a preparation method thereof. Background technique [0002] Many antineoplastic drugs have limited therapeutic effects due to weak penetration in tumor tissue sites and toxic side effects on normal cells at high doses. Usually in solid tumors, drugs can only penetrate into the area of ​​3-5 cell diameters near the tumor blood vessels. develop drug resistance. At present, many nanocarriers modified by targeting molecules (such as targeting polypeptide RGD, transferrin, folic acid, etc.) can carry drugs and accumulate in tumor sites, but still only a small amount of drugs can pass through vascular endothelial cells into tumor tissues and penetrate into the tumor parenchyma away from the tumor vessels. Therefore, how to effectively penetrate the blood vessel wall and penet...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K47/42A61K45/00A61K31/704A61K31/337A61P35/00
Inventor 梁兴杰魏妥柳娟
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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