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Disulfide bond-containing redox sensitive drug delivery system as well as preparation method and application thereof

A delivery system and sensitive technology, applied in the field of redox-sensitive drug delivery system and its preparation, can solve problems such as fracture

Pending Publication Date: 2021-05-18
XINXIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, disulfide bonds can exist stably in normal cells but break in tumor cells

Method used

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  • Disulfide bond-containing redox sensitive drug delivery system as well as preparation method and application thereof
  • Disulfide bond-containing redox sensitive drug delivery system as well as preparation method and application thereof
  • Disulfide bond-containing redox sensitive drug delivery system as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6

[0051] Polymer Poloxamer-b-PCL was prepared by ring-opening polymerization. With Poloxamer188 as the initiator, stannous octoate (Sn(Oct) 2 ) or tin triflate (Sn(oTf) 2 ) is a catalyst, which is prepared by reacting under anhydrous and oxygen-free conditions, and specific examples are as follows:

[0052]

Embodiment 1

[0054] Add 1.6g (0.2mmol) dry poloxamer188 (number average molecular weight 8000), 1.6g (14.0mmol) ε-caprolactone and 200μL stannous octoate into the dry reaction tube, vacuumize, fill with nitrogen, and repeat the operation three times. It was then placed in an oil bath at 140° C. for 10 h and then terminated. Finally, the product was dissolved in 6 mL of dichloromethane, then precipitated in glacial ether, and the product was obtained by suction filtration, and vacuum-dried at room temperature for 24 hours to obtain the polymer Poloxamer188-b-PCL.

Embodiment 2

[0056] Add 1.6g (0.2mmol) dry poloxamer188 (number average molecular weight 8000), 3.2g (28.0mmol) ε-caprolactone and 200μL stannous octoate into the dry reaction tube, vacuumize, fill with nitrogen, and repeat the operation three times. It was then placed in an oil bath at 140° C. for 10 h and then terminated. Finally, the product was dissolved in 6 mL of dichloromethane, then precipitated in glacial ether, and the product was obtained by suction filtration, and vacuum-dried at room temperature for 24 hours to obtain the polymer Poloxamer188-b-PCL.

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Abstract

The invention discloses a disulfide bond-containing redox sensitive drug delivery system as well as a preparation method and application thereof. A chemical structural general formula of the redox sensitive drug delivery system is shown in the description, wherein Drug is a drug containing amino or hydroxyl; and m ranges from 75 to 85, n ranges from 25 to 30, and p ranges from 10 to 35. The invention also specifically discloses the preparation method of the disulfide bond-containing redox sensitive drug delivery system and the application of the disulfide bond-containing redox sensitive drug delivery system to preparation of brain-targeted antitumor drugs. The development of the prepared redox sensitive drug delivery system not only provides an efficient chemical drug delivery system for clinic, but also provides a new thought and strategy for tumor microenvironment intelligent response type drugs.

Description

technical field [0001] The invention belongs to the technical field of preparation of pharmaceutical dosage forms and nano-medicines, and in particular relates to a redox-sensitive drug delivery system containing disulfide bonds, a preparation method and application thereof. Background technique [0002] Chemotherapy is one of the most common treatment methods for cancer. It mainly uses chemical drugs to inhibit the growth or spread of cancer cells in the patient's body, so as to achieve the purpose of treating cancer. However, many chemotherapeutic drugs have disadvantages such as low solubility, poor stability, high cytotoxicity and poor pharmacokinetic properties. Chemotherapy drugs are generally added with ethanol and Tween-80 as cosolvents when they are used clinically. However, these co-solvents are very likely to cause adverse reactions such as hemolysis, nephrotoxicity, neurotoxicity and cardiotoxicity, and may cause death in severe cases. Therefore, the applicatio...

Claims

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Application Information

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IPC IPC(8): A61K47/59A61K9/51A61K31/337A61K31/704A61K47/34A61P35/00B82Y5/00B82Y30/00B82Y40/00
CPCA61K47/59A61K31/704A61P35/00A61K31/337A61K9/5153B82Y5/00B82Y30/00B82Y40/00
Inventor 史永利马伟伟侯雪艳杨雪王霄
Owner XINXIANG MEDICAL UNIV
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