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Paclitaxel loaded sustained release nano fiber and preparation method and use thereof

A technology of nanofibers and paclitaxel, which is applied in the fields of fiber chemical characteristics, wet spinning method, and pharmaceutical formulations, can solve the problems of side effects, adverse effects of paclitaxel, and reduced drug efficacy, and achieve the effect of reducing toxic and side effects and simple preparation process

Inactive Publication Date: 2009-04-01
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these nanofibers prepared by electrospinning a simple mixture of drug and polymer, due to the rapid phase separation caused by the electrospinning process, the drug is easily distributed on the surface of the fiber or aggregated together, resulting in a burst release of the drug.
This drug release mode may cause side effects and reduce the efficacy of the drug in oral administration, which is unfavorable for the utilization of anticancer drugs such as paclitaxel

Method used

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  • Paclitaxel loaded sustained release nano fiber and preparation method and use thereof
  • Paclitaxel loaded sustained release nano fiber and preparation method and use thereof
  • Paclitaxel loaded sustained release nano fiber and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] (1) preparation polylactic acid (PLA) concentration is the solution of 0.06 g / ml, solvent used is the mixed solvent of hexafluoroisopropanol, trifluoroethanol or chloroform and acetone;

[0029] (2) preparing paclitaxel concentration is the solution of 10 mg / ml, the solvent used is trifluoroethanol;

[0030] (3) Add a 2.5ml outer syringe to the (1) solution, add a 2.5ml inner syringe to the (2) solution, and adjust the inner and outer layer speeds to 0.2 ml / hour and 0.4 ml / hour respectively, using a No. 9 needle The right-angled flat opening is used as the inner spinneret, the outer spinneret is 10mm, the applied voltage is 15KV, and the fiber is received at a place 10cm directly below the needle tip with a grounded aluminum foil.

[0031] The average diameter of gained drug-loaded fiber is 175mm, see figure 1 .

Embodiment 2

[0033] (1) preparation polyε-caprolactone (PCL) concentration is the solution of 0.04 g / ml, solvent used is the mixed solvent of hexafluoroisopropanol, trifluoroethanol or chloroform and acetone;

[0034] (2) preparing paclitaxel concentration is the solution of 10 mg / ml, the solvent used is trifluoroethanol;

[0035] (3) Add a 2.5ml outer syringe to the (1) solution, add a 2.5ml inner syringe to the (2) solution, adjust the speed of the inner and outer layers to 0.3ml / hour and 0.5ml / hour respectively, and use a No. 9 needle system The right-angled flat opening is used as the inner spinneret, the outer spinneret is 10mm, the applied voltage is 12KV, and the fiber is received at a place 15cm directly below the needle tip with a grounded aluminum foil.

[0036] The average diameter of the obtained drug-loaded fiber is 90nm, and the transmission electron microscope (TEM) test results are shown in figure 2 .

Embodiment 3

[0038] (1) preparation of lactide and caprolactone copolymer [P(LLA-CL)] is a solution of 0.08 g / ml, and the solvent used is a mixed solvent of hexafluoroisopropanol, trifluoroethanol or chloroform and acetone;

[0039] (2) preparing paclitaxel concentration is the solution of 19 mg / ml, the solvent used is trifluoroethanol;

[0040] (3) Add a 2.5ml outer syringe to the (1) solution, add a 2.5ml inner syringe to the (2) solution, and adjust the inner and outer layer speeds to be 0.4 ml / hour and 1.2 ml / hour respectively. The right-angled flat opening is used as the inner spinneret, the outer spinneret is 10mm, the applied voltage is 20KV, and the fiber filament is received at 19cm directly below the needle tip with a grounded aluminum foil.

[0041] The average diameter of the obtained drug-loaded fiber is 1.43 μm, the drug-loaded amount of the prepared drug-loaded fiber is 7%, and the encapsulation efficiency is 96.9%. The sustained-release behavior of the prepared drug-loaded...

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Abstract

The invention relates to a paclitaxel-loaded sustained release nano-fibre material which comprises the components of bio-degradable polymer material and pure paclitaxel, the mol ratio of which is 1.33 to 10. The diameter of the nano-fibre is 90nm to 1.44micrometer, and the drug-loading rate can be regulated within the range of 0 percent to 100 percent. The preparation of the nano-fibre comprises the steps as follows: (1) the bio-degradable polymer material is solved in organic solvent and stirred to be solved completely to obtain lamella spinning solution A; (2) the white pure paclitaxel powder is solved in trifluoroethanol and stirred to be solved completely to obtain core spinning solution B; (3) clear transparent solutions A and B are respectively added into two injectors; the speed of a microinjection pump, the voltage of a static generator and the receiving distance between a grounded aluminum foil and a spinning needle are adjusted, and unordered drug-loaded nano-fibre is obtained by a coaxial electrostatic spinning technology. A nanometer control release system composed by the drug-loaded nano-fibre effectively controls the sustained release of the drug and is applied to the preparation of the drug for remedying malignant tumor.

Description

technical field [0001] The invention belongs to the field of nanofiber preparation, in particular to a paclitaxel-loaded slow-release nanofiber, a preparation method and application thereof. Background technique [0002] Paclitaxel (trade name: taxol) is a natural anti-cancer raw material extracted from yew or yew trees. It is a white crystal powder, insoluble in water, and easily soluble in organic solvents such as chloroform and acetone. Its anti-tumor mechanism is to induce and promote the polymerization of tubulin into microtubules, and at the same time inhibit the depolymerization of the formed microtubules to generate stable microtubule bundles. The normal dynamic regeneration of microtubule bundles is blocked, and cells cannot form normal mitotic spindles during mitosis, thereby inhibiting cell division and proliferation. Its unique anti-tumor mechanism has a unique therapeutic effect on breast cancer, ovarian cancer and non-small cell cancer, and has been widely use...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/34A61K35/00D01D5/06D01F6/58D01F6/78D01F6/96
Inventor 莫秀梅黄慧华张鹏云刘晓锋高蔡玖
Owner DONGHUA UNIV
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