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Docetaxel-loaded nanoporous network fibers prepared by high-voltage electrospinning and their applications

A technology of high-voltage electrospinning and docetaxel, which is applied in spinning solution preparation, fiber treatment, filament/thread forming, etc., can solve the problems of inconvenient clinical medication, obvious adverse reactions, and low medication safety, and achieve Good biodegradability, good biocompatibility, effect of increasing specific surface area

Active Publication Date: 2016-08-24
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the dosage form on the market in China is injection. Although the curative effect of clinical medication is remarkable, the adverse reactions are also obvious at the same time. The solvent system can cause adverse reactions such as allergic reactions, and gastrointestinal reactions such as nausea, vomiting, or diarrhea may occur; due to the non-selective distribution of the drug, it will cause adverse reactions such as neurotoxicity, musculoskeletal toxicity, and neutropenia. In addition, Tween-80 also has slight hemolytic property and high viscosity. It needs pre-administration of antihistamines and glucocorticoids for clinical medication, which will bring great pain to patients, and it is inconvenient for clinical medication and the safety of medication Low

Method used

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  • Docetaxel-loaded nanoporous network fibers prepared by high-voltage electrospinning and their applications
  • Docetaxel-loaded nanoporous network fibers prepared by high-voltage electrospinning and their applications
  • Docetaxel-loaded nanoporous network fibers prepared by high-voltage electrospinning and their applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The viscosity-average molecular weight after vacuum drying with a mass ratio of 77:15:8 is 6×10 4 Polypropylene carbonate, viscosity average molecular weight is 6×10 4 The polycaprolactone pellets were mixed with docetaxel, and 0.15% titanium tetrachloride and 0.15% lithium bromide based on the total mass of the previous three materials, and then added chloroform: ethyl acetate: DMSO at a ratio of 80:3:17 A mixed solution with a concentration of 10% is prepared in a mixed solvent; the prepared mixed solution is placed in an electrospinning device connected to a needle with an inner diameter of 0.7mm, and the temperature is 18°C, the humidity is 50%, and the voltage is 17KV. / h injection into fibers, the formed nanofibers are collected by a turntable with a rotating speed of 250 rpm, and the distance between the needle point and the receiving turntable is 18cm; the obtained nanofibers are put into ultrapure water for 30 minutes, repeated 3 times, to fully remove For the...

Embodiment 2

[0035] The viscosity-average molecular weight after vacuum drying in a mass ratio of 85:10:5 is 5×10 4 Polypropylene carbonate with a viscosity average molecular weight of 1.5×10 5 Polycaprolactone pellets are mixed with docetaxel and 0.2% titanium tetrachloride based on the total mass of the previous three materials, and then added to acetone: ethyl acetate: DMF as a mixed solvent of 75:5:20 to prepare A mixed solution with a concentration of 13% was prepared; the prepared mixed solution was placed in an electrospinning device connected to a needle with an inner diameter of 0.8mm, and injected at a flow rate of 7ml / h at a temperature of 20°C, a humidity of 55%, and a voltage of 18KV. The formed nanofibers are collected by a rotating disk with a rotating speed of 300 rpm, and the distance between the needle point and the receiving rotating disk is 20 cm; the resulting nanofibers are put into ultrapure water for ultrasonic treatment for 10 minutes, and repeated 6 times to fully...

Embodiment 3

[0037] The viscosity-average molecular weight after vacuum drying with a mass ratio of 70:20:10 is 8×10 4 Polypropylene carbonate with a viscosity average molecular weight of 1×10 5 The polycaprolactone pellets are mixed with docetaxel and 0.5% lithium bromide based on the total mass of the previous three materials, and then added in chloroform: ethyl acetate: DMF in a mixed solvent of 88:2:10 to prepare a concentration of 7% mixed solution; place the prepared mixed solution in an electrospinning device connected to a needle with an inner diameter of 0.6mm, and inject it into fibers at a flow rate of 4ml / h at a temperature of 18°C, a humidity of 45%, and a voltage of 15KV. The nanofibers are collected by a turntable with a rotating speed of 200 rpm, and the distance between the needle point and the receiving turntable is 18cm; the resulting nanofibers are put into ultrapure water for ultrasonic treatment for 20 minutes, and repeated 4 times to fully remove lithium bromide in t...

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Abstract

The invention discloses a loaded docetaxel nano-pore containing network fiber prepared through high-voltage electrostatic spinning. The loaded docetaxel nano-pore containing network fiber is prepared by mixing polypropylene carbonate, polycaprolactone and docetaxel in a mass ratio of (45-98):(1-40):(1-15), and a conductive metal salt which accounts for 0.2-0.5% of the total mass of the three above materials in a high-voltage electrostatic spinning manner. An electron microscope image shows that the fiber consists of a great amount of nano-pore networks which are communicated with one another, and the specific surface area of the fiber is 130-211m<2> / g. The invention further discloses application of the loaded docetaxel nano-pore containing network fiber in chemotherapy after gliomas operation. The nano-pore networks which are communicated with one another are formed on the surface and inside the fiber disclosed by the invention, the specific surface area of the fiber is greatly increased, the release velocity and the accumulation release amount of a loaded medicine DOC can be also increased, the infiltration depth of the medicine in tumor is remarkably increased, a relatively good anti-tumor effect can be achieved, and furthermore, due to good biocompatibility and biodegradability, and the fiber can be used as a partial slow-release chemotherapeutic medicine in chemotherapy after malignant brain glioma operation, and the preparation method is simple and controllable.

Description

technical field [0001] The invention belongs to the technical field of high-voltage electrospinning fiber and its application, and in particular relates to a docetaxel-loaded nanopore fiber prepared by high-voltage electrospinning and its application. Background technique [0002] More than 60% of primary brain tumors in adults are gliomas. This is a very harmful malignant tumor with high morbidity and mortality. The survival period calculated from the initial diagnosis is only 9-9. 12 months. During the survival period, patients will also lose various functions, such as movement disorders, epilepsy, visual disorders, language disorders, etc., and their quality of life is extremely poor. Although the patients were treated with surgery, radiotherapy and chemotherapy, tumor recurrence occurred almost without exception in the patients. In the past 20 years, there has been no significant progress in the treatment of glioma. At present, the main treatment options are surgical ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): D01F8/14D01F1/10D01D1/02D01D5/00A61K31/337A61K47/34A61P35/00
Inventor 郭刚王跃龙仝爱平周良学魏于全
Owner SICHUAN UNIV
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