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Nano-medicine of biogenic macrocyclic molecule and preparation method of nano-medicine

A technology of nano-drugs and macrocyclic molecules, which can be applied to medical preparations with non-active ingredients, polymer compounds with non-effective ingredients, medical preparations containing active ingredients, etc. It can solve the problem of loss of tumor self-protection barrier and short circulation time in the body , damage to organ functions and other issues, to achieve good anti-tumor effect, excellent anti-tumor performance, and the effect of inhibiting the ring opening of lactone

Inactive Publication Date: 2019-01-29
NORTHWESTERN POLYTECHNICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Chemotherapy is to use chemotherapeutic drugs to kill cancer cells to achieve the purpose of treatment, but most of the chemotherapeutic drugs have many problems in the clinical use process, such as poor water solubility and stability, high toxicity, poor distribution selectivity, lack of targeting and The short circulation time in the body not only has low curative effect, but also causes serious side effects, damages the functions of important organs such as the heart, liver, lung, kidney, and bone marrow, destroys the immune system, and leads to the loss of the body's self-protection barrier against tumors. Suffering brings pain

Method used

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  • Nano-medicine of biogenic macrocyclic molecule and preparation method of nano-medicine
  • Nano-medicine of biogenic macrocyclic molecule and preparation method of nano-medicine
  • Nano-medicine of biogenic macrocyclic molecule and preparation method of nano-medicine

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Embodiment 1

[0052] This embodiment provides a kind of nanomedicine of biological source macrocyclic molecule (the nanomedicine number of the biological source macrocyclic molecule provided by this embodiment is SN38-ND), which comprises SN38 and transports phospholipid nanodiscs of SN38, and the phospholipid nanodisks are The two MSPs are connected head-to-tail to the outside of the phospholipid molecule - DMPC. The helical conformations of the two MSPs are parallel to the phospholipid molecule, and the hydrophobic residues of the MSP are located inside the helical conformation.

[0053] The present embodiment provides a method for preparing a nanomedicine of a biological source macrocyclic molecule, comprising the following steps:

[0054] 100 mg of DMPC was dissolved in 10 mL of a mixed solution of chloroform and methanol (chloroform: methanol = 3:1, v / v). Divide into 10 parts, dry in vacuum for 4h, use N 2 Blow dry slightly and store at -20°C. When using, take 1 portion of DMPC, the ...

Embodiment 2-4

[0058] The nano-drugs of bio-derived macrocyclic molecules provided in Examples 2-4 have the same basic structure as the nano-drugs of bio-derived macrocyclic molecules provided in Example 1, except that the raw materials used are different. The basic operation of the preparation method of the nano-medicine of the bio-derived macrocyclic molecule provided in Examples 2-4 is the same as the preparation method of the nano-medicine of the bio-derived macrocyclic molecule provided in Example 1, except that the specific operating conditions are different.

Embodiment 2

[0060] The nano-medicine of biological source macrocyclic molecule adopts phosphatidylcholine as the phospholipid molecule.

[0061] Every milligram of phospholipid molecules is dissolved in a mixed solution of 0.15 milliliters of chloroform and methanol, the concentration of the phospholipid molecular solution is 8 mg / mL, and the buffer is 18 mM, pH=3.0 sodium acetate buffer solution. The concentration of the drug solution is 4mg / mL, the volume ratio of the drug solution to the phospholipid molecular solution is 1:3, the shaking temperature is 20°C, and the shaking time is 5 hours. The concentration of the protein solution was 4 mg / mL, the volume ratio of the protein solution to the first mixed solution was 1:1.25, and the ultrasonic temperature was 22°C.

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Abstract

The invention relates to the field of pharmacy, in particular to a nano-medicine of a biogenic macrocyclic molecule and a preparation method of the nano-medicine. The nano-medicine of the biogenic macrocyclic molecule comprises 7-ethyl-10-hydroxycamptothecin and a phospholipid nanodisk transporting the 7-ethyl-10-hydroxycamptothecin, and the phospholipid nanodisk comprises a hydrophobic surface facing interior lipid and a hydrophilic surface facing outwards. The nano-medicine has excellent anti-tumor properties, negligible general toxicity and long-term immunotoxicity. The preparation method is simple in operation and mild in reaction conditions, and the nano-medicine can be rapidly prepared and obtained.

Description

technical field [0001] The invention relates to the field of pharmacy, and in particular to a nano-medicine of a biological source macrocyclic molecule and a preparation method thereof. Background technique [0002] As one of the largest public health problems in the world, malignant tumors have seriously threatened human life and health and become the second killer of human beings in the new century. Chemotherapy is to use chemotherapeutic drugs to kill cancer cells to achieve the purpose of treatment, but most of the chemotherapeutic drugs have many problems in the clinical use process, such as poor water solubility and stability, high toxicity, poor distribution selectivity, lack of targeting and The short circulation time in the body not only has low curative effect, but also causes serious side effects, damages the functions of important organs such as the heart, liver, lung, kidney, and bone marrow, destroys the immune system, and leads to the loss of the body's self-p...

Claims

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Application Information

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IPC IPC(8): A61K31/4745A61K47/24A61K47/42A61P35/00
CPCA61K31/4745A61K47/24A61K47/42A61P35/00
Inventor 葛岩潘铁铮沈鑫金林尚洁王杨鑫戚震辉
Owner NORTHWESTERN POLYTECHNICAL UNIV
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