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A kind of Tiancimycin liposome and its preparation method and application

A technology of liposomes and divasin, applied in liposomes, the application of liposomes in anti-tumor in vivo, can solve problems such as multidrug resistance, achieve significant targeting, improve poor solubility, The effect of enhancing the antitumor effect

Active Publication Date: 2022-08-05
HAYAO CIHANG PHARM CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no research on nano-nano drug delivery of Tiancimycin. The use of nanotechnology to deliver Tiancimycin drug provides a new way to develop new anti-tumor drugs and solve the problem of multi-drug resistance in tumors.

Method used

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  • A kind of Tiancimycin liposome and its preparation method and application
  • A kind of Tiancimycin liposome and its preparation method and application
  • A kind of Tiancimycin liposome and its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0051] Godcin lipid system preparation

[0052] Called 30mg of soybean phospholipids, 14mg of hydrogenated soybean phospholipids, 15mg of cholesterol, DSPE-PEG2000 10mg, TNM A400 μL (1 mg / ml of methanol liquid) in 5ml of dichloromethane, placed in a rotating and evaporating bottle, reducing the rotation and evaporation and the film. Essence Take a 5ml PBS water solution, place it in the firing bottle of the film, rotate the membrane hydration, the ice water bath ultrasonic dispersed 15min, ultrafiltration centrifugal tube (MW 3500) ultrafiltration centrifugation (4000rpm) 15min, it can be milk light Liposuction solution. Test the particle size of the lipomin lipids of 93nm, and the Zeta potential -4.5MV.

Embodiment 2

[0054] Targeted Tiancinin Liposure System Preparation

[0055] It is called to take 30mg of soybean phospholipids, hydrogenated soybean phospholipids 14 mg, cholesterol 15mg, DSPE-PEG2000 10mg, DSPE-PEG-CRGD 6mg, TNM A 400 μL (1 mg / ml of methanol liquid), and placed in rotation and evaporation In the bottle, the pressure rotation and evaporation are evenly forming the film. Take a 5ml PBS water solution, place it in the firing bottle of the film, rotate the membrane hydration, the ice water bath ultrasonic dispersed 15min, ultrafiltration centrifugal tube (MW 3500) ultrafiltration centrifugation (4000rpm) 15min, it can be milk light Liposuction solution. Testing targeted Tiancin lipids of 99nm, Zeta potential -5.1MV.

Embodiment 3

[0057] Test in vitro release test of lipomycin lipid body

[0058] Experimental method: Cut small dialysis bags (MW 3500), boil in boiling water for 10 minutes, and leave them in a pure water solution for soaking. In the bag, the two ends are tightly, and the dialysis bag is placed in the 20ml PBS buffer solution (0.5 % SDS) at a constant temperature shaking bed at 37 ° C at 200R / min. Take 1ml of samples at the specified time point, and HPLC detects the content of heavenlycin. After each sampling, the dialysis solution is 1ml. In vitro release experimental results such as figure 1 The results show that the accumulated release of the first 60H of the freeliestin reached 99 %, and the heavenlycedin lipids (LIP-TNM A) under physiological conditions (pH 7.4, 37 ° C, 0.5 % SDS) at 48 at 48 Suddenly released within hours, and the release degree is less than 45 %.

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Abstract

A kind of diocinycin liposome and its preparation method and application. The present invention relates to a kind of liposome and cRGD peptide-modified targeting liposome for the drug delivery of diocinomycin as well as its preparation and application. The present invention can overcome the shortcoming of poor water solubility of tinsomycin, can improve the anti-tumor effect of tinsomycin in vivo, and improve the effect of treating malignant tumor, and at the same time, the targeting liposome modified by cRGD peptide has good targeting property and remarkable anti-tumor effect. . The invention is simple in preparation and low in economic cost, provides a new way for promoting the clinical application of benzoanthraquinone enediyne diacetylmycin and the like, and also provides a variety of solutions for clinically solving the problem of tumor drug resistance, and can be widely used in the development of new drugs and pharmaceutical fields.

Description

Technical field [0001] The present invention involves liposomes and specifically involves liposomes and preparation methods containing godlin. The invention also involves the application of liposomes containing lipomycin in the body in the body, which belongs to the field of biomedical. Background technique [0002] Cancer is the most fatal human disease in the world, with more than 15 million new cancer cases every year in the world. Chemotherapy is the main cancer treatment method except surgery, radiotherapy, immunotherapy, etc. Although these therapeutic agents show relatively satisfactory results, they also have many shortcomings, including poor pharmacokinetics, non -specific differences, and low targeted capabilities. Poor solubility and specificity are considered to be the main obstacle to the treatment of drugs for cancer treatment. Therefore, it is urgent to overcome these shortcomings to improve the efficiency of the treatment of tumors. Sending toxic drugs to cancer c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/4748A61K47/24A61K47/28A61K47/18A61P35/00
CPCA61K9/127A61K9/0019A61K31/4748A61K47/24A61K47/28A61K47/18A61P35/00
Inventor 段燕文黄勇冯雪琼
Owner HAYAO CIHANG PHARM CO LTD
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