Response type small molecular peptide nano drug-loading carrier

A nano-drug-carrying and carrier technology, which can be applied to inactive components of polymer compounds, peptides, microcapsules, etc., can solve problems such as refractory degradation and immune response, achieve low synthesis cost, convenient purification, and avoid potential biological toxicity and immunity. source effect

Inactive Publication Date: 2019-04-26
WEIFANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Nano-drug carriers formed with polymers as raw materials have problems such as refractory degradation and easy to cause immune reactions in the body.

Method used

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  • Response type small molecular peptide nano drug-loading carrier
  • Response type small molecular peptide nano drug-loading carrier
  • Response type small molecular peptide nano drug-loading carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: Ac-VVVVVVKKK-NH 2 Preparation of peptides

[0047] Step 1. Distill N,N-dimethylformamide (DMF) and piperidine (Piperidine) solvents

[0048] The purchased DMF solution was distilled under reduced pressure at 60°C to obtain pure DMF solvent; the purchased piperidine was heated to reflux for 1-2 hours, and the boiling point temperature (106°C) fraction was received to obtain pure piperidine solvent.

[0049] Step 2, preparation of amino acid, resin, activator, capping agent, deprotecting agent

[0050] Calculate and prepare 0.25mM Ac-VVVVVVKKK-NH on the polypeptide solid-phase synthesizer 2 Amounts of amino acids and other reagents required:

[0051] Lys (lysine): 1.04g dissolved in 11mL DMF;

[0052] Val (valine): 2.18g dissolved in 32mL DMF;

[0053] Resin (loaded at 0.6mmol / g): 0.417g;

[0054] Activator: Diisopropylcarbodiimide (DIC): 17mL;

[0055] Activated base: 17-(Acetyloxy)-3-Methoxy-20-oxo-pregna-3,5-diene-6-carboxaldehyde (Oxyma, CAS No.: 57361...

Embodiment 2

[0061] Example 2: Ac-VVVVVVKKK-NH 2 Preparation of drug-loaded carrier

[0062] Weigh 0.519mg (0.5mmol / L) peptide Ac-VVVVVVKKK-NH 2 , adding 1 mL of PBS buffer solution, ultrasonication for 5 min, and standing at room temperature for 4 h, the observation results of TEM and SEM showed that nanoparticle self-assembly had been formed at this time ( figure 1 , figure 2 ).

Embodiment 3

[0063] Example 3: Ac-VVVVVVKKK-NH 2 Detection of self-assembled morphology of drug-loaded carriers in PBS buffer

[0064] The specific detection method is as follows:

[0065] Examination of self-assembled morphologies (TEM, SEM) in PBS buffer.

[0066] TEM: The model of TEM used in the experiment is JEM 1400Plus transmission electron microscope. Take 30 μL of the sample to be tested obtained in Example 2 and drop it on the PARAFILM sealing film to form a droplet, put the copper mesh covered with the carbon support film on the droplet to absorb for 30s to 3min, remove the copper mesh, and absorb the excess liquid on the surface with filter paper , and then use 2% uranyl acetate aqueous solution to negatively stain the carbon support membrane with the sample adsorbed for 1 to 3 minutes, absorb the excess dye solution with filter paper, leave it to dry at room temperature, and use TEM to test, the electron acceleration voltage It is 120KV. The results showed that the peptide...

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Abstract

The invention provides polypeptide with a structural formula of Ac-VVVVVVKKK-NH2 and discloses construction and preparation methods and application of a peptide nano drug-loading carrier. The Ac-VVVVVVKKK-NH2 polypeptide is self-assembled in a PBS (Phosphate Buffered Saline) solution to form a nanosphere shape; and a polypeptide nanosphere can be used as the drug-loading carrier to embed a fat-soluble drug. The nanosphere provided by the invention and formed by self-assembly of polypeptide molecules can be cracked and collapsed into nano-fibers through adding plasma amine oxidase, so that thefat-soluble drug is effectively released; and the nanosphere is an ideal nano drug-loading material and has important significance to life health of human beings.

Description

technical field [0001] The invention relates to the technical field of nano drug-loaded carrier and its preparation, in particular to an enzyme-responsive small molecular peptide nano drug-loaded carrier, its preparation method and its application. Background technique [0002] Nano-drug carriers formed from polymers are difficult to degrade and easily cause immune reactions in the body. Using amino acids as raw materials to form nanoparticles as a drug carrier has the advantages of easy degradation. Amino acids are widely present in the body, generally do not introduce the body's immune response, and have low cytotoxicity. Some amino acids can undergo chemical reaction changes under the catalysis of enzymes, and have enzyme responsiveness, which can be used to construct intelligent peptide nano-drug carriers. Contents of the invention [0003] The object of the present invention is to provide an enzyme-responsive small molecule peptide nano drug carrier, its preparation...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K9/51A61K47/42A61K31/7052
CPCA61K9/5169A61K31/7052C07K7/06
Inventor 白靖琨龚中英
Owner WEIFANG MEDICAL UNIV
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