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PH-response drug-loaded self-assembly aquagel-formed polypeptide, preparation method and use

A hydrogel and self-assembly technology, which can be used in the preparation method of peptides, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of poor oral bioavailability, insufficient tissue distribution, unstable circulation, etc. To achieve the effects of no toxic side effects, short length and simple preparation method

Active Publication Date: 2021-06-18
乐普制药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although nanoparticles have many advantages as drug carriers, there are still many shortcomings, such as poor oral bioavailability, unstable circulation, insufficient tissue distribution, toxicity, etc.

Method used

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  • PH-response drug-loaded self-assembly aquagel-formed polypeptide, preparation method and use
  • PH-response drug-loaded self-assembly aquagel-formed polypeptide, preparation method and use
  • PH-response drug-loaded self-assembly aquagel-formed polypeptide, preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A preparation method of pH-responsive self-assembled polypeptide hydrogel is carried out in two steps.

[0030] 1. Synthesis of polypeptide chain

[0031] The invention provides a pH-responsive self-assembled polypeptide prepared by the existing solid-phase synthesis method. Include the following steps:

[0032] The first step, swelling of RINK resin

[0033] The RINK resin that takes by weighing is placed in the reactor of 150ml, after dichloromethane (DCM) soaks 2 hours, fully washes resin with the nitrogen-dimethylformamide (DMF) of 3 times of resin volume, then drains and waits for use.

[0034] The second step, removal of Fmoc protecting group

[0035] Add a certain amount of 20% piperidine solution into the polypeptide reactor, filter the reaction solution after the reaction, and remove the Fmoc protecting group on the resin. After deprotection, wash with DMF, and then drain. A resin free of the initially attached Fmoc protecting group is obtained.

[0036]...

Embodiment 2

[0049] A pH-responsive self-assembled polypeptide hydrogel, the preparation method of which is:

[0050] Dissolve the synthesized peptide in water, vortex until dissolved to form a peptide solution with a concentration of 10mg / ml, adjust the pH value of the peptide solution (pH5.8, pH7.4) with 0.1M NaOH, and let it stand at room temperature for 30min , observe and record whether the polypeptide solution forms a transparent and clear hydrogel in different pH ranges.

[0051] The results of gelation of the polypeptide hydrogel prepared in this example under different pH conditions are as follows: figure 1 As shown, under the neutral condition of pH 7.4, the polypeptide solution can form a stable transparent clear hydrogel, the glass vial is inverted, the hydrogel remains stable, and the gel structure will not be damaged; while in the acidic pH of 5.8 Under these conditions, the peptide solution cannot form a stable hydrogel structure. It shows that under normal physiological c...

Embodiment 3

[0053] The secondary structure of the polypeptide in Example 1 is tested by circular dichroism, and the experimental steps are as follows:

[0054] 1) Prepare a 0.1mg / ml peptide solution;

[0055] 2) adjust the pH value of the polypeptide solution to 7.4 and 5.8 respectively;

[0056] 3) Add 15ul sample to a 0.1cm quartz cuvette;

[0057]4) Place the quartz cuvette in the circular dichroism spectrometer, set the scanning wavelength range to 190-260nm, the bandwidth to 1nm, the response time to 1s, the scanning speed to 100nm / min, and the temperature to 25°C;

[0058] 5) After scanning, transfer the data out and make a graph.

[0059] Among them, the circular dichroism detection results are as follows figure 2 shown. The secondary conformation ratios of polypeptides in different buffer solutions are shown in Table 1.

[0060] Table 1 The secondary conformation ratios of polypeptides in different pH buffer solutions

[0061]

[0062] figure 2 The results show that un...

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Abstract

The invention discloses a pH-response drug-loaded self-assembly aquagel-formed polypeptide, a preparation method and use. An amino acid sequence of the polypeptide is Ile-Glu-Ile-Ile-Ile-Orn. Aquagel is formed through dissolving the polypeptide in an aqueous solution, carrying out swirling until the polypeptide is dissolved so as to form a polypeptide solution, adjusting a pH, and carrying out standing gelatination at room temperature. The obtained polypeptide aquagel is good in biocompatibility, high in mechanical properties and low in toxic or side effects; and the polypeptide aquagel disclosed by the invention has relatively high sensitivity to the pH, the aquagel loading doxorubicin hydrochloride is implanted to a focus region in an injection manner, the drug-loaded polypeptide aquagel can achieve targeted sustained / controlled release of a drug under the stimulation of an acidulous environment of a tumor, the antitumor treatment effect of the drug is improved, and the drug-loaded polypeptide aquagel is free of toxic or side effects on normal tissue.

Description

technical field [0001] The invention relates to a biomedical material, in particular to a pH-responsive drug-loaded self-assembled polypeptide to form a hydrogel, a preparation method and an application. Background technique [0002] Breast cancer is the most common malignant tumor in women all over the world, and it has become a major public health problem in contemporary society. Although significant progress has been made in the treatment of breast cancer, the cytotoxicity and drug resistance of traditional chemotherapy drugs still pose great challenges to the effective treatment of breast cancer. Therefore, finding an efficient intratumoral targeted drug delivery system to achieve sustained targeted release of drugs has become an important problem that we urgently need to solve. [0003] At present, many researchers are studying new anti-tumor drug carriers for drug delivery. However, there are still many problems, such as poor solubility of drugs, non-specific biodist...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/04C07K1/06C07K1/14A61K9/06A61K31/704A61K47/42A61P35/00
CPCC07K7/06A61K9/06A61K47/42A61K31/704A61P35/00Y02P20/55
Inventor 周闻舞罗诗瑶葛亮
Owner 乐普制药科技有限公司
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