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Drug-polypeptide self-assembled nanoparticles and preparation method thereof

A nanoparticle and self-assembly technology, which can be used in drug combination, drug delivery, and pharmaceutical formulations. It can solve the problems of early release, low water solubility, and low structural stability, and achieve low toxicity and high water solubility.

Pending Publication Date: 2021-12-21
SHENZHEN INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the drug delivery systems of liposomes, condition-responsive nanomaterials and polymers are mostly reported, which solve the problems of drug targeting, biocompatibility and safety to a certain extent, but most of these nano-preparations are hydrophobic Coating / encapsulation of sexual small molecule drugs, the structural stability is not high, and leakage or early release often occurs during delivery in the blood, causing safety problems
Therefore, it is necessary to develop a drug that can simultaneously solve the problems of triptolide's high toxicity, low water solubility, and unstable nano-drug structure.

Method used

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  • Drug-polypeptide self-assembled nanoparticles and preparation method thereof
  • Drug-polypeptide self-assembled nanoparticles and preparation method thereof
  • Drug-polypeptide self-assembled nanoparticles and preparation method thereof

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preparation example Construction

[0041] A preparation method of drug-polypeptide self-assembled nanoparticles, comprising the steps of:

[0042] (1) Synthetic prodrug, prodrug is synthesized by hydrophobic small molecule drug, phenylalanine dipeptide, hydrophilic group, described hydrophobic small molecule drug is triptolide, camptothecin, paclitaxel, doxorubicin At least one of the hormones, the hydrophilic group is glucosamine.

[0043] Including the following steps:

[0044] a. prepare amino-phenylalanine dipeptide-glucosamine;

[0045] b. Preparation of carboxyl hydrophobic small molecule drugs;

[0046] c. Obtain the product hydrophobic small molecule drug-phenylalanine dipeptide-glucosamine.

[0047] (2) The prodrug is added into the aqueous solution to self-assemble to obtain nanoparticles.

Embodiment 1

[0049] Example 1 Synthesis of prodrug: triptolide-diphenylalanine-glucose.

[0050] The preparation method of triptolide-diphenylalanine-glucose comprises the following steps, such as figure 1 Shown:

[0051] (1) tert-butoxycarbonyl-phenylalanine dipeptide-glucosamine (Boc-Phe-Phe-OH), 1-ethyl-3-(3-di Methylaminopropyl) carbodiimide and N-hydroxysuccinimide are dissolved together;

[0052] (2) Anhydrous dimethylformamide (DMF) solution dissolved with glucosamine and triethylamine (TEA) is added dropwise to the above solution;

[0053] (3) After the above mixture was evaporated under reduced pressure for 20-28 hours, the product tert-butoxycarbonyl-phenylalanine dipeptide-glucosamine (BOC-FF-AG) was obtained;

[0054] (4) Dissolve tert-butoxycarbonyl-phenylalanine dipeptide-glucosamine (BOC-FF-AG) in a mixture of equal volumes of anhydrous dichloromethane and trifluoroacetic acid, and stir at room temperature for 3- 6 hours;

[0055] (5) After the above solution is evapora...

Embodiment 2

[0062] Example 2 Triptolide Nanomedicine In Vivo Drug Toxicity Analysis

[0063] Male BALB / c mice were randomly divided into four groups, and were injected intravenously with PBS buffer solution (PBS), triptolide (triptolide), triptolide nano-medicines (TPNs) and erythrocyte membrane Bionic triptolide nano-medicine (manRTPNs), the drug-polypeptide self-assembled nanoparticles in the present invention are Figure 7 Membrane-inspired triptolide nanomedicines (manRTPNs) in.

[0064] After continuous injection for one week, all mice were euthanized, blood was collected for blood routine examination and biochemical parameter measurement, and major organs such as heart, liver, spleen, lung and kidney were excised and H&E stained for histological examination and analysis . The result is as Figure 7 As shown, the number of blood cells including leukocytes, erythrocytes and platelets decreased significantly after the former drug of triptolide was treated, indicating that it has sid...

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Abstract

The invention provides a drug-polypeptide self-assembled nanoparticles and a preparation method thereof. The particles are formed by self-assembling prodrug molecules under a hydrophobic effect after the prodrug molecules are synthesized by hydrophobic small-molecule drugs, phenylalanine dipeptide and hydrophilic glycosamine groups. The prodrug molecules are obtained after successful structural modification is carried out on the hydrophobic small-molecule original drugs, and the original drugs are wrapped by a compact spherical structure formed by self-assembly of the prodrug molecules, so that the original drugs have low toxicity and high water solubility. Compared with other drug-loaded nano-carriers, the nanoparticles solve the problems of low drug loading capacity and low encapsulation efficiency, have obvious advantages in drug loading capacity, and can be used for preparing anti-inflammatory or anti-tumor drugs.

Description

technical field [0001] The invention relates to the field of nanomedicine, in particular to a drug-polypeptide self-assembled nanoparticle and a preparation method thereof. Background technique [0002] Hydrophobic small molecule drugs, such as triptolide, camptothecin, paclitaxel, doxorubicin, etc., have significant immunosuppressive, anti-inflammatory and anti-tumor activities. They have been widely used in the treatment of inflammation and anti-tumor therapy. Recent experimental data show that some of these drugs (such as triptolide) not only have broad-spectrum anti-tumor activity and tumor resistance reversal, but also can enhance the anti-tumor effect of other therapies. However, the hydrophobic small molecule drugs listed above have the disadvantage of poor water solubility, which has greatly restricted the development and research of their anti-inflammatory or anti-tumor drugs. [0003] Among them, triptolide (Triptolide, TP), also known as triptolide, is one of th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/64A61K47/54A61K47/69A61K31/585A61K31/4745A61K31/337A61K31/704A61P35/00
CPCA61K47/64A61K47/549A61K47/6925A61K31/585A61K31/4745A61K31/337A61K31/704A61P35/00
Inventor 蔡林涛李三朋李菁龚萍
Owner SHENZHEN INST OF ADVANCED TECH
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