TPGS-reduced albumin nanoparticle preparation entrapped with taxol and preparation method

A technology of albumin nanoparticles and paclitaxel, which is applied in the field of preparation and preparation of paclitaxel-encapsulated protein-polymer conjugates, can solve the problems of changing the pharmacokinetic characteristics of tumor drugs, low efficiency and high toxicity, and achieves good tumor targeting properties, high drug loading, and improved therapeutic efficacy

Inactive Publication Date: 2016-06-01
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

P-gp protein inhibitors have also been studied to solve this problem, but small molecule inhibitors have many problems such as low efficiency and high toxicity, changing the pharmacokinetic characteristics of tumor drugs, and have not been widely used.

Method used

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  • TPGS-reduced albumin nanoparticle preparation entrapped with taxol and preparation method
  • TPGS-reduced albumin nanoparticle preparation entrapped with taxol and preparation method
  • TPGS-reduced albumin nanoparticle preparation entrapped with taxol and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Preparation of paclitaxel-loaded TPGS-reduced albumin nanoparticle preparation

[0035] (1) Weigh 0.1g (0.065mmol) of TPGS, 0.013g (0.013mmol) of succinic anhydride and 0.08g (0.065mmol) of DMAP, dissolve in 5ml of anhydrous dichloromethane, react at room temperature for 24h under nitrogen protection, and rotate to evaporate Dichloromethane was removed, dissolved in 5ml of pure water, placed in a dialysis bag with a molecular weight of 1000, dialyzed with pure water / ethanol (3:1, V / V) aqueous solution for 24 hours, and lyophilized to obtain TPGS-COOH.

[0036] Weigh 200mg of BSA, add 10ml of PBS buffer (pH8.0) to dissolve, add DTT, the amount added is 5 times the molar amount of disulfide bonds in BSA (about 0.04g), react for 4h, use fresh boiling water for dialysis for 24h, freeze-drying Get Re-BSA.

[0037]Weigh 69 mg of TPGS-COOH, dissolve it in 5 ml of DCM, add 0.01 g of EDC, 0.006 g of NHS (molar ratio 1:1.2:1.2), react for 8 hours, dry the DCM by rotary...

Embodiment 2

[0041] Example 2 Changes in drug loading and drug loading efficiency of TPGS-reduced albumin nanoparticles loaded with paclitaxel

[0042] (1) Weigh 0.1g (0.065mmol) of TPGS, 0.013g (0.013mmol) of succinic anhydride and 0.08g (0.065mmol) of DMAP, dissolve in 5ml of anhydrous dichloromethane, react at room temperature for 24h under nitrogen protection, and rotate to evaporate Dichloromethane was removed, dissolved in 5ml of pure water, placed in a dialysis bag with a molecular weight of 1000, dialyzed with pure water / ethanol (3:1, V / V) aqueous solution for 24 hours, and lyophilized to obtain TPGS-COOH.

[0043] Weigh 200mg of BSA, add 10ml of PBS buffer (pH8.0) to dissolve, add DTT, the amount added is 5 times the molar amount of disulfide bonds in BSA (about 0.04g), react for 4h, use fresh boiling water for dialysis for 24h, freeze-drying Get Re-BSA.

[0044] Weigh 69 mg of TPGS-COOH, dissolve it in 5 ml of DCM, add 0.01 g of EDC, 0.006 g of NHS (molar ratio 1:1.2:1.2), react...

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Abstract

The invention relates to a TPGS-reduced albumin nanoparticle preparation entrapped with taxol and a preparation method. According to the preparation, TPGS-reduced albumin is synthesized, and then taxol, TPGS-reduced albumin, water for injection and the like are used for preparing the TPGS-reduced albumin nanoparticle preparation entrapped with taxol. The preparation can form nanoparticles with a high drug loading capacity and improve enrichment of a drug in tumors through passive targeting, and meanwhile the carrier material achieves a certain multi-drug resistance resisting effect and plays a synergic anti-cancer role.

Description

technical field [0001] The invention relates to a drug-loaded preparation and a preparation method, in particular to a paclitaxel-loaded protein-polymer conjugate preparation and a preparation method. Background technique [0002] Cancer is one of the major diseases that endanger human health at present. According to the World Health Organization, between 2005 and 2015, 84 million people died of cancer. At the same time, the number of cancer cases in the world is increasing rapidly, and it is expected to increase from 14 million in 2012 to 19 million in 2025. 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, and the compound growth rate in China from 2008 to 2013 was 20.4%, much higher than the global level. [0003] Chemotherapy i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/337A61K47/42A61K47/34A61P35/00
CPCA61K9/5169A61K9/5146A61K31/337
Inventor 陈方城刘建平葛亮朱家壁
Owner CHINA PHARM UNIV
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