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Beaded nanofiber loaded with paclitaxel and preparation method thereof

A nanofiber, paclitaxel technology, applied in fiber processing, fiber chemical characteristics, rayon manufacturing and other directions, can solve the problems of uncontrollable drug release time and rate, unable to change the appropriate rate, large diameter of microsphere drug, etc. The effect of drug burst release, improving drug efficiency and good biocompatibility

Active Publication Date: 2018-03-09
XIAMEN TASMAN BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Aiming at the phenomenon of burst release, some scholars have developed a coaxial spinning drug loading method. The fiber prepared by this spinning method has less toxic and side effects, and alleviates the phenomenon of drug burst release to a certain extent, but the release time and rate of the drug cannot be determined. control, it is impossible to change the appropriate rate according to the type of drug loaded; at the same time, this method does not pretreat the drug, and there is likely to be drug inactivation
In order to avoid drug inactivation, the drug is often pretreated to form a microsphere structure with a protective layer. The diameter of the treated microsphere drug is large, and the nanofiber cannot effectively carry this type of drug. The sustained release effect is poor, and the preparation process is complicated.

Method used

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  • Beaded nanofiber loaded with paclitaxel and preparation method thereof
  • Beaded nanofiber loaded with paclitaxel and preparation method thereof
  • Beaded nanofiber loaded with paclitaxel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] 1) Prepare 14wt% polycaprolactone (PCL, molecular weight is 8×10 4 Da) solution, the solvent used is obtained by mixing the first solvent dichloromethane and the second solvent N,N-dimethylformamide with a mass ratio of 10:4;

[0034] 2) prepare 6wt% polyethylene glycol (PEG, molecular weight is 6 * 10 3 Da) solution, the solvent used is obtained by mixing the first solvent dichloromethane and the second solvent N,N-dimethylformamide with a mass ratio of 10:4;

[0035] 3) Mix the polycaprolactone solution in step 1) with the polyethylene glycol solution in step 2) according to the mass ratio of 1:1, then add paclitaxel to it to make the final concentration 5wt%, stir evenly, Obtain paclitaxel solution;

[0036] 4) Add the paclitaxel solution in step 3) into a 2.5mL syringe, and perform electrospinning at a spinning voltage of 6kV and a spinning flow rate of 0.5mL / h (the schematic diagram of the electrospinning device is shown in figure 1 shown, the same below), the h...

Embodiment 2

[0039] 1) prepare 14wt% polycaprolactone (molecular weight is 8 * 10 4 Da) solution, the solvent used is obtained by mixing the first solvent dichloromethane and the second solvent N,N-dimethylformamide with a mass ratio of 10:4;

[0040] 2) prepare 6wt% polyethylene glycol (molecular weight is 6 * 10 3 Da) solution, the solvent used is obtained by mixing the first solvent dichloromethane and the second solvent N,N-dimethylformamide with a mass ratio of 10:4;

[0041] 3) Mix the polycaprolactone solution in step 1) with the polyethylene glycol solution in step 2) according to the mass ratio of 1:1, then add paclitaxel to it to make the final concentration 3wt%, stir evenly, Obtain paclitaxel solution;

[0042] 4) Add the paclitaxel solution in step 3) into a 2.5mL syringe, and perform electrospinning at a spinning voltage of 6kV and a spinning flow rate of 0.9mL / h. The needle of the syringe is the level of the spinneret and the flat receiver The distance is 15cm, the flat r...

Embodiment 3

[0045] 1) prepare 14wt% polycaprolactone (molecular weight is 8 * 10 4 Da) solution, the solvent used is obtained by mixing the first solvent dichloromethane and the second solvent N,N-dimethylformamide with a mass ratio of 10:4;

[0046] 2) prepare 6wt% polyethylene glycol (molecular weight is 1 * 10 4 Da) solution, the solvent used is obtained by mixing the first solvent dichloromethane and the second solvent N,N-dimethylformamide with a mass ratio of 10:4;

[0047] 3) Mix the polycaprolactone solution in step 1) with the polyethylene glycol solution in step 2) according to the mass ratio of 1:1, then add paclitaxel to it to make the final concentration 6wt%, stir evenly, Obtain paclitaxel solution;

[0048] 4) Add the paclitaxel solution in step 3) into a 2.5mL syringe, and perform electrospinning at a spinning voltage of 6kV and a spinning flow rate of 0.6mL / h. The needle of the syringe is the level of the spinneret and the flat receiver The distance is 15cm, and the fl...

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Abstract

The invention discloses a paclitaxel loaded catenulate nano fiber and a preparation method thereof. At first, catenulate nano fiber is prepared, then paclitaxel is loaded on the beads to form a drug sustain-released system, and thus slow releasing of paclitaxel can be effectively controlled. Furthermore, the biocompatibility is good, the drug encapsulation rate is high, and the activity is strong. The provided dosage form of paclitaxel has the advantages of little side and toxic effect and sustained-release function, and can be applied to preparation of drugs for treating malignant tumors.

Description

technical field [0001] The invention relates to the field of drug sustained and controlled release carriers, in particular to a beaded nanofiber loaded with paclitaxel and a preparation method thereof. Background technique [0002] Paclitaxel has a unique anticancer mechanism and high anticancer activity, and is widely used in the treatment of various tumors such as ovarian cancer, breast cancer, and lung cancer, with a high cure rate. Due to its poor solubility in water, paclitaxel injection is currently used in clinical medicine, which needs to be dissolved in a mixed solvent of polyoxyethylene castor oil and absolute ethanol to increase water solubility, and polyoxyethylene castor oil releases histamine when degraded in the body, which will cause Different degrees of allergic reactions can also cause granule release and demyelination changes in nerve cells and aggravate the peripheral neurotoxicity of paclitaxel. [0003] In order to reduce toxicity and improve its effic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): D01F8/14D01F8/16D01F1/10D01D5/00A61P35/00
CPCD01D5/003D01F1/10D01F8/14D01F8/16
Inventor 汤须崇徐祥雷廷平肖尚晨寇新月赵雯
Owner XIAMEN TASMAN BIO TECH
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