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A kind of targeting preparation and preparation method of albumin nanoparticles co-loaded with doxorubicin and trail

A technology of albumin nanoparticles loaded with doxorubicin, applied in peptide/protein components, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of easy drug resistance, cell apoptosis, etc., and achieve increased accumulation , reduce the effect of toxic and side effects

Inactive Publication Date: 2018-06-19
SHENYANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

TRAIL is prone to drug resistance when used alone, and synergistic or additive effects can be seen in combination with chemotherapy drugs (such as etoposide, cisplatin, doxorubicin and 5-fluorouracil), which can lead to apoptosis

Method used

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  • A kind of targeting preparation and preparation method of albumin nanoparticles co-loaded with doxorubicin and trail
  • A kind of targeting preparation and preparation method of albumin nanoparticles co-loaded with doxorubicin and trail
  • A kind of targeting preparation and preparation method of albumin nanoparticles co-loaded with doxorubicin and trail

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Preparation of albumin nanoparticle-targeted formulations co-loaded with doxorubicin and TRAIL

[0039] (1) Take BSA to make a 2% (g / ml) aqueous solution, and adjust the pH to 8.0 with 1 mole per liter of sodium hydroxide solution. Take 1 ml of BSA solution, add 4 ml of 0.02% doxorubicin hydrochloride ethanol solution dropwise to it with stirring, at a rate of 10 ml / min, to obtain a drug-containing albumin solution. Then, add 4% glutaraldehyde ethanol solution dropwise to the drug-containing albumin solution under stirring, continue to stir for 2 hours, then transfer to a rotary evaporator, and rotary evaporate at 40°C for 20 minutes under vacuum to remove ethanol. The obtained product was centrifuged at 10°C and 14,000 rpm for 10 minutes, discarded the centrifuged supernatant, washed and centrifuged twice with distilled water repeatedly, and discarded the supernatant to obtain nanoparticles. Then add distilled water to the nanoparticles and vortex to dispers...

Embodiment 2

[0043] Example 2 Preparation of albumin nanoparticle-targeted formulations co-loaded with doxorubicin and TRAIL

[0044] (1) Take BSA to make a 1% (g / ml) aqueous solution, and adjust the pH to 8.0 with 1 mole per liter of sodium hydroxide solution. Take 1 ml of BSA solution, add 4 ml of 0.01% ethanol solution of doxorubicin dropwise to it under stirring, at a speed of 10 ml / min, to obtain a drug-containing albumin solution. Then, add 4% glutaraldehyde ethanol solution dropwise to the drug-containing albumin solution under stirring, continue to stir for 2 hours, then transfer to a rotary evaporator, and rotary evaporate at 40°C for 20 minutes under vacuum to remove ethanol. The obtained product was centrifuged at 10°C and 14,000 rpm for 10 minutes, discarded the centrifuged supernatant, washed and centrifuged twice with distilled water repeatedly, and discarded the supernatant to obtain nanoparticles. Then add distilled water to the nanoparticles and vortex to disperse to obta...

Embodiment 3

[0047] Example 3 Preparation of Drug-loaded Albumin Nanoparticles Targeting Folate Receptor and Tumor pH-Sensitive Release

[0048] (1) Take BSA to make a 5% (g / ml) aqueous solution, and adjust the pH to 8.0 with 1 mole per liter of sodium hydroxide solution. Take 1 ml of BSA solution, add 4 ml of 0.05% ethanol solution of doxorubicin dropwise to it under stirring, at a speed of 10 ml / min, to obtain a drug-containing albumin solution. Then, add 4% glutaraldehyde ethanol solution dropwise to the drug-containing albumin solution under stirring, continue to stir for 2 hours, then transfer to a rotary evaporator, and rotary evaporate at 40°C for 20 minutes under vacuum to remove ethanol. The obtained product was centrifuged at 10°C and 14,000 rpm for 10 minutes, discarded the centrifuged supernatant, washed and centrifuged twice with distilled water repeatedly, and discarded the supernatant to obtain nanoparticles. Then add distilled water to the nanoparticles and vortex to dispe...

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Abstract

A targeted preparation of albumin nanoparticles co-loaded with doxorubicin and TRAIL and its preparation method, the preparation is composed of doxorubicin hydrochloride DOX·HCl, human tumor necrosis factor apoptosis ligand TRAIL, bovine serum albumin BSA, Albumin nanoparticle targeted drug delivery system loaded with doxorubicin and TRAIL made of polyethyleneimine PEI, carboxymethyl chitosan-folate conjugate CMCS-FA, water for injection, cross-linking agent, etc. Preparation of folic acid-targeted albumin nanoparticles co-encapsulating doxorubicin and TRAIL by preparing doxorubicin-loaded albumin nanoparticles, carboxymethyl chitosan‑folate conjugate (CMCS‑FA) Mediated active targeting and tumor pH-sensitive drug release improve the enrichment of drug carriers in tumors; the loaded doxorubicin and TRAIL can produce synergistic anticancer effects and have a strong killing effect on cancer cells (including drug-resistant cells) .

Description

technical field [0001] The invention relates to a drug-loaded preparation and a preparation method, in particular to an albumin nanoparticle targeting preparation and a preparation method of co-loading doxorubicin and TRAIL. Background technique [0002] According to the "Global Cancer Report 2014" released by the World Health Organization, the global cancer cases will show a rapid growth trend, from 14 million in 2012 to 19 million in 2025, and the number will increase to 24 million in 2035 people. Nearly half of the new cases are in Asia, most of which are in China. China has 3.07 million new cancer patients and 2.2 million deaths every year, accounting for 21.9% and 26.8% of the global total respectively. Therefore, the market for antineoplastic drugs has grown rapidly in recent years, with a compound growth rate of 7.2% globally from 2008 to 2013, and a compound growth rate of 20.4% in China, much higher than the global growth rate. [0003] The defect of current treat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K38/17A61K47/22A61K47/42A61P35/00A61K31/704
Inventor 张岩李洪仁李锋
Owner SHENYANG UNIV
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