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Drug delivery carrier containing TGF (transforming growth factor) alpha-Saporin and preparation method of carrier

A drug delivery carrier and carrier technology, which is applied in the field of drug delivery carrier containing TGFα-Saporin and the preparation of drug delivery carrier, can solve the problems of smooth muscle cell proliferation, damage, and vascular endothelialization, and achieve the purpose of inhibiting smooth muscle cell proliferation and promoting damaged vascular endothelialization , the effect of preventing restenosis of surgical vessels

Inactive Publication Date: 2014-07-16
杨军
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to provide a drug delivery carrier containing TGFα-Saporin and a preparation method of the delivery carrier, so as to solve the problem that the delivery carrier in the prior art cannot simultaneously selectively inhibit the proliferation of smooth muscle cells and promote the endothelialization of damaged blood vessels. question

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  • Drug delivery carrier containing TGF (transforming growth factor) alpha-Saporin and preparation method of carrier
  • Drug delivery carrier containing TGF (transforming growth factor) alpha-Saporin and preparation method of carrier
  • Drug delivery carrier containing TGF (transforming growth factor) alpha-Saporin and preparation method of carrier

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preparation example Construction

[0072] Another aspect of the present invention also provides a method for preparing the above-mentioned drug delivery carrier containing TGFα-Saporin, the method comprising the following steps: sequentially immersing the carrier body in the drug solution, pulling out and drying to obtain the drug delivery carrier containing TGFα-Saporin drug carrier.

[0073] The specific steps are as follows: when the administration carrier containing TGFα-Saporin is composed of a TGFα-Saporin drug layer and a polymer layer, at this moment, the carrier body is first immersed in the TGFα-Saporin drug solution, and after staying for 1 to 15 minutes, the The carrier is pulled out and the resulting carrier is dried. Then immerse the dried carrier in the high molecular polymer solution, soak for 1-15 minutes, pull out, and dry the obtained carrier to be the drug delivery carrier containing TGFα-Saporin. Obviously, in what order the carrier body is immersed in which solution, the drug solution of ...

Embodiment 1

[0092] Preparation method of derivatized TGFα

[0093] 1) 20 mg of TGFα was dissolved in 2.67 ml of boric acid buffer. Add 267ul of SMPT (0.48mg / m1) dissolved in dimethylformamide to make the molar ratio of SMPT to TGFα excessive by 2.5 times. In order to keep the solubility of SMPT, the amount of dimethylformamide in the reaction system should be at 10% (V / V), and stirred at room temperature for 1 hour to obtain the first derivatized TGFα.

[0094] 2) The first derivatized TGFα was passed through a SephadexG25 column (30*1.5cm) and equilibrated with phosphoric acid-EDTA buffer, the first eluted peak was collected, dried and concentrated by nitrogen blowing or filtered through molecular sieves to obtain purified derivatized TGFα.

[0095] Preparation method of the first product of activated Saporin

[0096] 10 mg of Saporin was dissolved in 7 ml of phosphoric acid-EDTA buffer and reacted with solid TCEP at room temperature. The end point of the reaction was about 30 minutes...

Embodiment 2

[0102] Preparation method of derivatized TGFα

[0103] 1) 20 mg of TGFα was dissolved in 2.67 ml of boric acid buffer. Add 267ul of SMPT (0.48mg / ml) that is dissolved in dimethylformamide, make the molar ratio of SMPT and TGFα exceed 2.5 times, in order to keep the solubility of SMPT, the amount of dimethylformamide in the reaction system is at 10% (V / V), and stirred at room temperature for 1 hour to obtain the first derivatized TGFα.

[0104] 2) The first derivatized TGFα was passed through a SephadexG25 column (30*1.5cm) and equilibrated with phosphoric acid-EDTA buffer, the first eluted peak was collected, dried and concentrated by nitrogen blowing or filtered through molecular sieves to obtain purified derivatized TGFα.

[0105] Preparation method of the first product of activated Saporin

[0106] 10 mg of Saporin was dissolved in 7 ml of phosphoric acid-EDTA buffer and reacted with solid DTT at room temperature. The end point of the reaction was about 30 minutes when t...

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Abstract

The invention provides a drug delivery carrier containing TGF (transforming growth factor) alpha-Saporin and a preparation method of the carrier. The drug delivery carrier comprises a carrier body and a drug coating, wherein the drug coating wraps the carrier body; the drug coating comprises at least one TGF alpha-Saporin drug layer wrapping the surface of the carrier body and at least one macromolecule polymer layer wrapping the outmost layer of the TGF alpha-Saporin drug layer. According to the drug delivery carrier, a common drug delivery carrier is coated with TGF alpha-Saporin which can selectively inhibit smooth muscle cell proliferation and promote endothelialization of injured vessels at the same time, and thus the coating stent can effectively inhibit vascular restenosis and lower the occurrence rates of post-stent implantation stent thrombosis and acute major adverse cardiovascular events.

Description

technical field [0001] The invention relates to the field of postoperative treatment of coronary heart disease, in particular to a drug delivery carrier containing TGFα-Saporin and a preparation method of the drug delivery carrier. Background technique [0002] Transforming growth factor-α (transforming growth factorα, TGFα) is a small molecule polypeptide produced by macrophages, brain cells and epidermal cells, which can induce epithelial or endothelial repair, and can promote the proliferation and differentiation of various cells. TGFα plays its role through the binding of the cell surface receptor epidermal growth factor receptor (EGFR). After binding to the epidermal growth factor high-affinity receptor, it undergoes a series of biological signal transduction to make the cell proliferate and synthesize the corresponding DNA. At the same time TGFα is also a powerful chemokine for endothelial cells, which can promote endothelial cell apology and repair. [0003] Saporin ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61L31/10A61L31/16C07K19/00C07K1/107
Inventor 杨军楮春余细勇罗健
Owner 杨军
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