Resveratrol and temozolomide double-medicine-loaded nanospheres, as well as application and preparation method thereof

A technology of resveratrol and temozolomide is applied in the field of anti-glioma double-drug nano-drug-loaded microspheres and the preparation thereof, which can solve the problems of affecting a wide range of applications, insufficient clinical efficacy, large oral dose and the like, and achieves the preparation method. Simple and easy, superior anti-tumor efficacy, enhanced synergistic effect

Inactive Publication Date: 2013-03-27
徐华娥 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to its rapid oral elimination, it is difficult to maintain an effective drug concentration in the brain
Simultaneously because its oral dose is relatively large, it is easy to produce certain side effects
For example, the incidence of severe nausea and vomiting (CTC grade 3 or 4) is 10 or 6, and it has a certain dose-dependent myelosuppressive toxicity, which has obvious limitations on clinical application
[0003] In addition, since temozolomide was used in the clinical treatment of glioma, many research results have shown that its clinical effective rate is less than 45%, and some patients have better short-term curative effect after application of temozolomide, but the long-term curative effect is not good, which seriously affects Its wide application in clinical
However, the above patents are all preparation methods of single-drug temozolomide or resveratrol nano-loaded microspheres, and the obtained single-drug nano-microspheres still cannot avoid the problems existing in monotherapy

Method used

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  • Resveratrol and temozolomide double-medicine-loaded nanospheres, as well as application and preparation method thereof
  • Resveratrol and temozolomide double-medicine-loaded nanospheres, as well as application and preparation method thereof
  • Resveratrol and temozolomide double-medicine-loaded nanospheres, as well as application and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Step 1, dispensing: Weigh 30g of temozolomide (TEM), 30g of resveratrol (RES) and 940g of drug-loaded materials according to the weight ratio of the raw material components, wherein the drug-loaded materials are polycaprolactone and polyethylene glycol Amphiphilic block copolymer polycaprolactone-polyethylene glycol (mPEG-PCL) synthesized by diol, in which: mPEG molecular weight is 4000, PCL molecular weight is 20000 (molecular weight is mainly distributed in this interval);

[0047] Step 2, drug dissolving: under normal temperature conditions, dissolve the raw material components such as 30g resveratrol (RES) and 940g drug-loaded material weighed in step 1 in a certain amount of acetone solvent (according to the weight of the components) Ratio, raw material component 80, acetone solvent 20); 30g temozolomide (TEM) weighed in step 1 was dissolved in a certain amount of distilled water at 45-50 degrees Celsius, (wherein according to the weight ratio of the components, tem...

Embodiment 2

[0054] Step 1, dispensing: Weigh 100g of temozolomide (TEM), 100g of resveratrol (RES) and 800g of drug-loaded materials according to the weight ratio of the raw material components, wherein the drug-loaded materials are polycaprolactone and polyethylene glycol Amphiphilic block copolymer polycaprolactone-polyethylene glycol (mPEG-PCL) synthesized by diol, in which: mPEG molecular weight is 4000, PLA molecular weight is 40000;

[0055] Step 2, drug dissolving: at room temperature, dissolve the raw material components such as 100g resveratrol (RES) and 800g drug-loaded material weighed in step 1 in a certain amount of ethanol solvent (according to the weight of the components) Ratio, raw material component 60, acetone solvent 40); Dissolve the 100g temozolomide (TEM) weighed in step 1 in a certain amount of distilled water at 45-50 degrees Celsius, wherein according to the weight ratio of the components, temozolomide 40, distilled water 60;

[0056] Step 3, preparation: add th...

Embodiment 3

[0062]Step 1, dispensing: Weigh 150g temozolomide (TEM), 150g resveratrol (RES) and 700g drug-loaded material according to the weight ratio of the raw material components, wherein the drug-loaded material is polycaprolactone and polyethylene glycol Amphiphilic block copolymer polycaprolactone-polyethylene glycol (mPEG-PCL) synthesized by diol, in which: mPEG molecular weight is 4000, PLGA molecular weight is 36000;

[0063] Step 2, drug dissolving: at room temperature, dissolve the raw material components such as 150g resveratrol (RES) and 700g drug-loaded material weighed in step 1 in a certain amount of acetone solvent (according to the weight of the components) Ratio, raw material component 50, acetone solvent 50); Dissolve 100g temozolomide (TEM) weighed in step 1 in a certain amount of distilled water at 45-50 degrees Celsius, wherein according to the weight ratio of the components, temozolomide 50, distilled water 50;

[0064] Step 3, preparation: add the resveratrol ob...

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Abstract

The invention discloses resveratrol and temozolomide double-medicine-loaded nanospheres, which are prepared by mixing temozolomide (TEM), resveratrol (RES) and a medicine-loading material, wherein the medicine-loading material is an amphiphilic segmented copolymer, namely, polycaprolactone-polyethyleneglycol (mPEG-PCL) or polylactic acid-polyethyleneglycol (mPEG-PLA) or polyglycolic acid-polyethyleneglycol (mPEG-PLGA) synthesised by polycaprolactone or polylactic acid or polyglycolic acid and polyethyleneglycol. The preparation method comprises the following steps of: dissolving the two raw material constituents, namely, the resveratrol (RES) and the medicine-loading material, in a water-soluble non-toxic organic solvent, and dissolving temozolomide in pure water, and stirring; filtering the obtained light-blue dispersion liquid by a microfiltration membrane having a mesh diameter of 220+30 nm to obtain anti-tumour double-medicine-loaded nanosphere solution having a particle diameter of 80-120 nm; and heat-drying or freeze-drying.

Description

technical field [0001] The invention relates to a medicine for treating glioma, in particular to a double-drug nano drug-loaded microsphere for anti-glioma and a preparation method thereof. Background technique [0002] Temozolomide was approved by the FDA in August 1991 for the treatment of refractory glioblastoma multiforme in adults and is a first-line drug for the treatment of malignant glioma. Its main dosage form is oral capsule preparation. After oral administration, the plasma drug concentration reaches its peak within 1 hour. It can be widely distributed throughout the body without liver metabolism, and can penetrate the blood-brain barrier and enter the cerebrospinal fluid central nervous system to achieve effective drug concentration. However, due to its rapid oral elimination, it is difficult to maintain an effective drug concentration in the brain. Simultaneously because its oral dose is relatively large, it is easy to produce certain side effects. For example...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4188A61K31/05A61K9/16A61K9/19A61P35/00
Inventor 王虹解卫平徐华娥李晓林
Owner 徐华娥
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