Amphiphilic polypeptide, heterozygous liposome and its preparation method, and drug-loaded heterozygous liposome and its preparation method

An amphiphilic and liposome technology, which is applied in the field of nanomaterials, can solve the problems of complex chemical reaction operations, high cost of peptide synthesis, and difficulty in ensuring utilization, and achieves simple preparation methods, high specificity, and good drug loading effect Effect

Inactive Publication Date: 2016-07-06
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

However, there are still disadvantages of relatively high cost of peptide synthesis when using peptides to design enzyme-responsive materials.
Moreover, when modifying materials, an excessive amount of peptides is usually required, which makes it difficult to ensure the utilization rate. At the same time, the chemical reaction operation is relatively complicated, and it is difficult to achieve mass production.

Method used

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  • Amphiphilic polypeptide, heterozygous liposome and its preparation method, and drug-loaded heterozygous liposome and its preparation method
  • Amphiphilic polypeptide, heterozygous liposome and its preparation method, and drug-loaded heterozygous liposome and its preparation method
  • Amphiphilic polypeptide, heterozygous liposome and its preparation method, and drug-loaded heterozygous liposome and its preparation method

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Experimental program
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preparation example Construction

[0040] In a second aspect, the present invention provides a method for preparing an enzyme-responsive hybrid liposome, the method comprising: contacting an amphiphilic polypeptide with a phospholipid, wherein the amphiphilic polypeptide is the amphiphilic peptides.

[0041] According to the method for preparing enzyme-responsive hybrid liposomes of the present invention, it should be particularly noted that since the amphiphilic polypeptide is the amphiphilic polypeptide of the present invention, therefore, regarding the present invention The aforementioned definition, scope and explanation of the amphipathic polypeptide are all applicable to the preparation method of the enzyme-responsive hybrid liposome of the present invention, and the present invention will not repeat them here.

[0042] According to the method for preparing enzyme-responsive hybrid liposomes of the present invention, the contact conditions may include: a pH value of 6-8, preferably 6.5-7.5.

[0043] Acco...

specific Embodiment approach

[0053] According to another preferred embodiment of the present invention, the preparation method of the enzyme-responsive hybrid liposome of the present invention comprises:

[0054] 1) mixing the enzyme-responsive amphiphilic polypeptide with a first solvent to obtain solution A; and dissolving the phospholipid and cholesterol in a second solvent to obtain solution B;

[0055] 2) contacting the solution A and solution B in step 1);

[0056] 3) Removing the solvent in the product obtained after the contact between the amphiphilic polypeptide and the phospholipid in step 2) by rotary evaporation to obtain the first product;

[0057] 4) dissolving the first product in step 3) with PBS buffer solution, followed by the first ultrasonic and centrifugal separation;

[0058] 5) Add the PBS buffer solution again to the white or milky white precipitate in the lower layer obtained after centrifugation in step 4), and then perform a second ultrasound to obtain enzyme-responsive hybrid ...

preparation example 1

[0101] This preparation example is used to synthesize the amphiphilic polypeptide of the structure shown in the formula (1) of the present invention, wherein n is 7, and the 7 amino acid residues constituting the polypeptide fragment that can be hydrolyzed by the enzyme are sequentially isoleucine residues, proline residues, valine residues, serine residues, leucine residues, arginine residues, and serine residues, and the isoleucine residue at the head end of the polypeptide fragment is related to the formula ( 1) The corresponding carboxyl group in the structure shown in the formula (1) is connected, and the serine residue at the end is connected with the corresponding amino group in the structure shown in formula (1).

[0102] According to the method provided in the literature (JingxiaoChen et al., Biomaterials, 2011, Vol32, 1678-1684), the amphiphilic polypeptide T1 represented by the formula (1) was synthesized.

[0103] According to mass spectrometry (time-of-flight mass...

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Abstract

The invention discloses an amphiphilic polypeptide, a heterozygous liposome and its preparation method, and a drug-loaded heterozygous liposome and its preparation method. The invention discloses the amphiphilic polypeptide with enzyme responsiveness. The amphiphilic polypeptide is shown in the structural formula (1) and in the structural formula (1), R represents amino acid residue, n is an integer of 4-10, n R groups are same or different and the n R groups form at least one polypeptide fragment hydrolyzed by an enzyme. The invention also provides the heterozygous liposome with enzyme responsiveness and a preparation method thereof. The preparation method comprises that the amphiphilic polypeptide contacts with phosphatide. The invention also provides the drug-loaded heterozygous liposome with enzyme responsiveness and its preparation method. The preparation method comprises that the amphiphilic polypeptide, a drug compound and phosphatide contacts. The drug carrier prepared from the amphiphilic polypeptide with enzyme responsiveness has the advantages of high specificity, good drug carrying effects, a moderate drug release rate and good stability. The preparation methods have simple processes and have low costs.

Description

technical field [0001] The present invention relates to the field of nanomaterial research, in particular, to an enzyme-responsive amphiphilic polypeptide, a method for preparing an enzyme-responsive hybrid liposome, and an enzyme-responsive hybrid liposome prepared by the method Liposome, a preparation method of drug-loaded hybrid liposome and drug-loaded hybrid liposome prepared by the method. Background technique [0002] In recent years, the development and research of nano-drug carriers has received extensive attention. Nano-drug carriers have many advantages, such as: nanoparticles are easy to prepare, modified and processed with good controllability, and can protect drugs, genes or functional molecules from degradation by the body or some enzymes, etc. Some nanoparticles, while acting as "carriers", also have the function of immune adjuvants. [0003] Liposome is an artificial vesicle structure. When liposome is in water, the hydrophilic head of phospholipid molecul...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08C07K1/107A61K9/127A61K47/42A61P35/00A61P43/00
Inventor 赵颖聂广军季天骄郎佳妍覃好
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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