Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Doxorubicin and itraconazole co-loaded nanoliposomes and preparation method thereof

An itraconazole nano- and nano-liposome technology, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations containing active ingredients, can solve the lack of evaluation results of in vivo tumor-bearing animals, insufficient treatment results Comprehensive evaluation of drug efficacy and toxic side effects, and normal tissue toxic side effects, etc., to achieve the effect of inhibiting vascular endothelial cell proliferation, improving tumor treatment effect, and inhibiting tumor angiogenesis

Active Publication Date: 2018-12-25
SICHUAN UNIV
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is used for tumor treatment through intravenous administration, and lacks tumor targeting, resulting in poor therapeutic effect on tumors and high toxicity to normal tissues.
2) The above two studies only reported the preliminary results of in vitro cells, and lacked the evaluation results of the treatment effect of tumor-bearing animals in vivo, so it is not enough to comprehensively evaluate the efficacy and side effects of drugs

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Doxorubicin and itraconazole co-loaded nanoliposomes and preparation method thereof
  • Doxorubicin and itraconazole co-loaded nanoliposomes and preparation method thereof
  • Doxorubicin and itraconazole co-loaded nanoliposomes and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The processing steps of the present embodiment are as follows:

[0037] (1) Preparation of itraconazole nanoliposomes

[0038] Take by weighing itraconazole 10g (2 mass parts), soybean lecithin (soybean phosphatidylcholine purity > 76%) 540g (108 mass parts), cholesterol 400g (80 mass parts), each raw material that weighs is dissolved together Form solution in the combination solvent that methanol and dichloromethane combine gained with volume ratio 1:2, the consumption of described combination solvent is limited to 1mg / L with soybean lecithin concentration in solution, remove solvent and obtain lipid film, the gained lipid film Soluble in 250mmol / L (NH 4 ) 2 SO 4 A suspension is formed in the solution, (NH 4 ) 2 SO 4 The amount of solution used is limited to the concentration of soybean lecithin in the suspension formed at 0.1 mg / mL. Ultrasonic the obtained suspension in a water bath at 30°C for 15 minutes, and ultrasonically with a probe at room temperature for ...

Embodiment 2

[0043] The processing steps of the present embodiment are as follows:

[0044] (1) Preparation of itraconazole nanoliposomes

[0045] Weigh itraconazole 100g (20 mass parts), phosphatidylglycerol 280g (56 mass parts), hydrogenated soybean phosphatidylcholine 420g (84 mass parts), cholesterol 150g (30 mass parts), polyethylene glycol modified Cholesterol 45g (9 mass parts), each raw material that weighs is dissolved in methanol and dichloromethane to form a solution in the combined solvent of the combination gained of volume ratio 1:2, the consumption of described combined solvent is based on the phospholipid (phospholipid) in the solution The total mass of acylglycerol and hydrogenated soybean phosphatidylcholine) concentration is limited to 200mg / L, and the solvent is removed to obtain a lipid film, and the gained lipid film is dissolved in 400mmol / L (NH 4 ) 2 SO 4 A suspension is formed in the solution, (NH 4 ) 2 SO 4 The amount of solution used is limited to the conce...

Embodiment 3

[0050] The processing steps of the present embodiment are as follows:

[0051] (1) Preparation of itraconazole nanoliposomes

[0052] Weigh itraconazole 20g (4 mass parts), phosphatidylserine 180g (36 mass parts), hydrogenated egg yolk phosphatidylcholine 400g (80 mass parts), cholesterol 100g (20 mass parts), polyethylene glycol modified Distearoylphosphatidylglycerol 100g (20 parts by mass), each weighed raw material is dissolved in the combined solvent obtained by combining methanol and chloroform with a volume ratio of 1:2 to form a solution, the amount of the combined solvent With the concentration of phospholipids (the total mass of phosphatidylserine and hydrogenated egg yolk phosphatidylcholine) in the solution being limited to 50 mg / L, remove the solvent to obtain a lipid film, and dissolve the gained lipid film in 300 mmol / L (NH 4 ) 2 SO 4 A suspension is formed in the solution, (NH 4 ) 2 SO 4 The amount of solution used is limited to the concentration of phosp...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
particle diameteraaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention provides doxorubicin and itraconazole common carrier nano-liposome which is mainly prepared from doxorubicin hydrochloride, itraconazole, phospholipids, other components, an ammonium sulfate solution and water for injection. The average grain diameter is 60-200 nm. The nano-liposome is prepared from, by mass, 1-40 parts of the doxorubicin hydrochloride, 1-20 parts of the itraconazole, 80-140 parts of the phospholipids and 20-100 parts of the other components; the other components are at least one of cholesterol, glycolipid and sitoesterol; the concentration of the ammonium sulfate solution is 100-400 mmol / L, and the water for injection is normal saline or glucose injection with the mass concentration of 5%. Medicine is endowed with a tumor tissue target ability through the lipidosome, tumor angiogenesis and tumor cell proliferation can be effectively restrained, and the toxic and side effects on normal tissue of the human body from the medicine are reduced.

Description

technical field [0001] The invention belongs to the technical field of medicaments, in particular to a liposome co-loaded with doxorubicin and itraconazole and a preparation method thereof. Background technique [0002] At present, significant progress has been made in the prevention and treatment of cancer, but due to the difficulty in early diagnosis of cancer and the lack of effective technical solutions for the treatment of cancer metastasis, curing cancer is still a difficult problem. The crux of the problem is that although anti-cell proliferation drugs can directly kill some tumor cells, the remaining tumor cells can continue to proliferate due to the support of surrounding blood vessels, and even metastasize through blood vessels or lymphatic vessels, resulting in failure of tumor treatment. In response to this problem, the global medical community has adopted "anti-tumor angiogenesis + anti-tumor cell proliferation" treatment schemes in recent years to achieve the g...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/496A61K31/704A61P35/00
Inventor 李莉顾忠伟贺晓丹
Owner SICHUAN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products