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Macrophage drug-loading preparation and preparation method thereof

A macrophage and drug-loading technology, which is applied in pharmaceutical formulations, anti-tumor drugs, drug combinations, etc., to achieve good anti-tumor activity and good tumor suppression effect

Active Publication Date: 2018-12-21
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drug encapsulation efficiency of the reported macrophage drug-loaded preparations is only 13.8%, which is far below the standard stipulated in the Chinese Pharmacopoeia

Method used

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  • Macrophage drug-loading preparation and preparation method thereof
  • Macrophage drug-loading preparation and preparation method thereof
  • Macrophage drug-loading preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Preparation of drug-loaded preparations of M1 macrophages loaded with doxorubicin

[0033] Preparation of fat-soluble doxorubicin:

[0034] (1) Weigh 20 mg of doxorubicin hydrochloride (purchased from Dalian Meilun Biotechnology Co., Ltd.) into a 100 ml round bottom flask, and add 20 ml of dichloromethane to fully dissolve it.

[0035] (2) Add 14.3mL of triethylamine according to the molar ratio of 1:3, and stir overnight at 25°C;

[0036] (3) Collect the product after 24 hours and place it in a dialysis bag for dialysis until the dialysate is clear and colorless;

[0037] (4) Collect the material in the dialysis bag and freeze-dry it to obtain dark red doxorubicin powder;

[0038] (5) Dissolve 1.630 mg of doxorubicin powder in 1 mL of DMSO to make a final concentration of 3 mmol / L.

[0039] Preparation of M1 macrophages:

[0040] (1) RAW264.7 cells (purchased from the Animal Experiment Center of Sun Yat-Sen University) were placed in high-glucose DMEM me...

Embodiment 2

[0046] Example 2: Preparation of drug-loaded preparations of M1 macrophages loaded with doxorubicin

[0047] Preparation of fat-soluble doxorubicin:

[0048] (1) Weigh 20mg of doxorubicin hydrochloride in a 100ml round bottom flask, add 20mL of dichloromethane to fully dissolve.

[0049] (2) Add 14.3mL of triethylamine according to the molar ratio of 1:3, and stir overnight at 25°C;

[0050] (3) Collect the product after 24 hours and place it in a dialysis bag for dialysis until the dialysate is clear and colorless;

[0051] (4) Collect the material in the dialysis bag and freeze-dry it to obtain dark red doxorubicin powder;

[0052] (5) Dissolve 2.445 mg of doxorubicin powder in 1 ml of DMSO to make a final concentration of 4.5 mmol / L.

[0053] Preparation of M1 macrophages:

[0054] (1) RAW264.7 cells were cultured in high-glucose DMEM medium containing 10% fetal bovine serum at 37°C and 5% CO 2 Subculture under the culture conditions.

[0055] (2) After 24 hours of pass...

Embodiment 3

[0060] Example 3: Preparation of drug-loaded preparations of M1 macrophages loaded with doxorubicin

[0061] Preparation of fat-soluble doxorubicin:

[0062] (1) Weigh 20 mg of doxorubicin hydrochloride (purchased from Dalian Meilun Biotechnology Co., Ltd.) into a 100 ml round bottom flask, and add 20 ml of dichloromethane to fully dissolve it.

[0063] (2) Add 14.3mL of triethylamine according to the molar ratio of 1:3, and stir overnight at 25°C;

[0064] (3) Collect the product after 24 hours and place it in a dialysis bag for dialysis until the dialysate is clear and colorless;

[0065] (4) Collect the material in the dialysis bag and freeze-dry it to obtain dark red doxorubicin powder;

[0066] (5) Dissolve 0.815 mg of doxorubicin powder in 1 mL of DMSO to make a final concentration of 1.5 mmol / L.

[0067] Preparation of M1 macrophages:

[0068] (1) RAW264.7 cells were cultured in high-glucose DMEM medium containing 10% fetal bovine serum at 37°C and 5% CO 2 Subcultu...

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Abstract

The invention relates to a macrophage drug-loading preparation and a preparation method thereof. The preparation method for the macrophage drug-loading preparation comprises the following steps: (1) enabling an anti-tumor drug to be dissolved in a solvent, and preparing an anti-tumor drug solution; (2) enabling macrophages to be suspended in a glucose solution of which a mass percent is (5+ / -1)%,to obtain macrophage suspension; (3) adding the anti-tumor drug solution to the macrophage suspension, and uniformly mixing; and (4) after culturing for 1.5-3.5 hours, centrifuging, and collecting a cell precipitate, to obtain the macrophage drug-loading preparation. The macrophage drug-loading preparation is high in encapsulation efficiency, long in drug-loading cell activity duration time, capable of slowly releasing a drug, and has good tumor targeting and inhibiting effects.

Description

technical field [0001] The invention relates to a targeted drug delivery preparation, in particular to a macrophage drug-loaded preparation and a preparation method thereof. Background technique [0002] Various cells in the body's circulatory system have different physiological functions, these functions include: long-lasting blood circulation life, transport capacity for endogenous substances and metabolites, tropism for sites of inflammation, crossing lipid biomembrane barriers, The ability to migrate between blood and tissues, homing or migrate to a specific pathological environment, these functions are becoming excellent conditions for it to be used as a drug carrier. The currently studied cell carriers include red blood cells, immune cells (neutrophils, macrophages and T lymphocytes) and stem cells. However, for large-scale production and use, the source and preparation process of red blood cells, neutrophils, lymphocytes and stem cells are the main problems hindering...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K45/00A61P35/00A61K39/00A61K35/15A61K47/46
CPCA61K9/5068A61K35/15A61K39/0011A61K45/00A61P35/00
Inventor 郭羚冯敏
Owner SUN YAT SEN UNIV
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