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Anti-tumor double-drug nano drug carrying microsphere and preparation method thereof

A nano-drug-loading and anti-tumor technology, applied in the field of anti-tumor drugs, can solve the problems of serious toxic and side effects such as liver and kidney toxicity and hematological toxicity, difficult to exert synergistic effects, and affect anti-tumor activity, and achieve superior anti-tumor efficacy. , to avoid individual aggregation, and the preparation method is simple and easy to implement.

Inactive Publication Date: 2014-09-10
孙亦彬
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] In 2009, the "Education Collection and Proceedings of the Third China Medical Oncology Conference" reported that cisplatin and tetrandrine (Tet) were loaded into polycaprolactone-polyethylene glycol nanospheres by double emulsion method , although the good anti-tumor activity of the drug-loaded microspheres has been confirmed in vitro, the toxic side effects such as liver and kidney toxicity and hematological toxicity are still serious after cisplatin is nanosized, which affects its further application.
In order to improve the oral bioavailability of paclitaxel, paclitaxel, tetrandrine (Tet) and cyclodextrin are co-filled into capsules. The elimination of the first pass, poor bioavailability, inability to achieve long-term effective blood drug concentration in the body and other difficult problems to solve. In addition, it is difficult for the two drugs to play a synergistic effect under the influence of the above factors after they are filled into capsules and taken orally, which in turn affects their Antitumor activity in patients

Method used

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  • Anti-tumor double-drug nano drug carrying microsphere and preparation method thereof
  • Anti-tumor double-drug nano drug carrying microsphere and preparation method thereof
  • Anti-tumor double-drug nano drug carrying microsphere and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0054] Step 1, dispensing: Weigh 30g of paclitaxel (Ptx), 30g of tetrandrine (Tet) and 940g of drug-loaded materials according to the weight ratio of raw material components, wherein the drug-loaded materials are polycaprolactone and polyethylene glycol Amphiphilic block copolymer polycaprolactone-polyethylene glycol (mPEG-PCL) synthesized by alcohol, wherein: mPEG molecular weight is 4000, PCL molecular weight is 20000;

[0055] Step 2, dissolving medicine: under normal temperature condition, raw material components such as 30g paclitaxel (Ptx), 30g tetrandrine (Tet) and 940g drug-loaded material taken in step 1 are dissolved in a certain amount of acetone solvent ( According to the weight ratio of components, raw material components 80%, acetone solvent 20%);

[0056] Step 3, dilution: the acetone solution obtained in step 2 is slowly added dropwise to a certain amount of distilled water under stirring conditions (the volume ratio of acetone solution and distilled water is 1...

Embodiment 2

[0061] Step 1, dispensing: Weigh 100g of paclitaxel (Ptx), 100g of curcumin (Cum) and 800g of drug-loaded material according to the weight ratio of the raw material components, wherein the drug-loaded material is a bismuth compound synthesized by polylactic acid and polyethylene glycol. Block-friendly copolymer polylactic acid-polyethylene glycol (mPEG-PLA), wherein: mPEG molecular weight 4000, PLA molecular weight 40000;

[0062] Step 2, drug dissolving: under normal temperature condition, raw material components such as 100g paclitaxel (Ptx), 100g curcumin (Cum) and 800g drug-loaded material taken in step 1 are dissolved in a certain amount of acetone solvent (according to group The weight proportion of part, raw material component 65%, acetone solvent 35%);

[0063]Step 3, dilution: slowly drop the acetone solution obtained in step 2 into a certain amount of distilled water (the volume ratio of acetone solution to distilled water is 1: 4.5) under stirring conditions, to obt...

Embodiment 3

[0068] Step 1, dispensing: Weigh 180g of paclitaxel (Ptx), 180g of resveratrol (Res) and 640g of the drug-loaded material according to the weight ratio of the raw material components, wherein the drug-loaded material is polyglycolic acid and polyethylene glycol Synthetic amphiphilic block copolymer polyglycolic acid-polyethylene glycol (mPEG-PLGA), wherein: mPEG molecular weight 4000, PLGA molecular weight 36000;

[0069] Step 2, drug dissolving: under normal temperature conditions, raw material components such as 180g paclitaxel (Ptx), 180g resveratrol (Res) and 640g drug-loaded material taken in step 1 are dissolved in a certain amount of acetone solvent ( According to the weight ratio of components, raw material components 50%, acetone solvent 50%);

[0070] Step 3, dilution: the acetone solution obtained in step 2 is slowly added dropwise to a certain amount of distilled water under stirring conditions (the volume ratio of acetone solution to distilled water is 1:5), and t...

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Abstract

The invention relates to an anti-tumor drug, in particular to an anti-tumor double-drug nano drug carrying microsphere and a preparation method thereof. The double-drug nano drug carrying microsphere disclosed by the invention is formed by mixing paclitaxel (Ptx), concordant remedies and drug carrying materials, wherein the concordant remedies are tetrandrine (Tet), or curcumin (Cum) or resveratrol (Res), the drug carrying material is amphiphilic block copolymer, namely polycaprolactone-polyethylene glycol (mPEG-PCL) or polylactic acid-polyethylene glycol (mPEG-PLA) or polyglycolic acid-polyethylene glycol (mPEG-PLGA), synthesized by polycaprolactone or polylactic acid or polyglycolic acid and polyethylene glycol. The preparation method disclosed by the invention comprises the steps of dosage, medicine dissolving, dilution, purification, filtering, drying or freeze drying and the like to obtain the anti-tumor double-drug nano drug carrying microsphere or finished freeze-drying product. According to the anti-tumor double-drug nano drug carrying microsphere and the preparation method thereof, the concordant remedies have the synergistic effect of reinforcing the tumor inhibiting capability of the paclitaxel so as to improve the pesticide effect of the double drugs for resisting tumor in a synergy manner.

Description

technical field [0001] The invention relates to an antitumor drug, in particular to an antitumor double-drug nano drug-loaded microsphere and a preparation method thereof. Background technique [0002] Today's anti-tumor drugs emerge in endlessly, but reducing the toxic and side effects of anti-tumor drugs is an urgent problem that needs to be solved. The following is the correct description of the names of each antineoplastic drug, that is, add (English abbreviation) after its Chinese name. Paclitaxel (Ptx) is currently a commonly used anti-tumor drug in clinical practice, but its toxic side effects on cancer patients and the increasing drug resistance of tumor cells have greatly restricted the clinical use of this drug. In view of the existing problems of paclitaxel single drug, the medical community further carried out nano-scale research on paclitaxel single drug. For example, paclitaxel is loaded into the amphiphilic block copolymer in the water phase to make nano dru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/19A61K31/337A61K31/4748A61K31/12A61K31/05A61K47/34A61P35/00
Inventor 李晓林刘宝瑞徐华娥孙亦彬
Owner 孙亦彬
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