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PCL-PLGA slow-release preparation and preparation method thereof

A technology of PCL-PLGA and sustained-release preparations, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve the problems of restricting the development of PLGA, poor mechanical toughness, and too short degradation cycle, etc. problems, achieve the effects of low cost, easy operation, and simple preparation equipment

Inactive Publication Date: 2018-02-27
HUAQIAO UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are many limitations in the application of PLGA, such as poor mechanical toughness and too short degradation cycle, which restrict the development of PLGA in the field of sustained-release preparations to a certain extent.

Method used

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  • PCL-PLGA slow-release preparation and preparation method thereof
  • PCL-PLGA slow-release preparation and preparation method thereof
  • PCL-PLGA slow-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] 1) Preparation of spinning solution:

[0031] In parts by volume, 9 parts of trifluoroethanol and 1 part of distilled water are mixed to prepare a spinning solvent; the PCL-PLGA polymer is added to the above spinning solvent and the concentration of the PCL-PLGA polymer in the spinning solvent is 10wt%; stirring at 25-30°C for 12 hours to fully dissolve the PCL-PLGA polymer; standing for defoaming for 2 hours to obtain a PCL-PLGA electrospinning solution;

[0032] Among them, in the PCL-PLGA polymer, the molecular weight of PCL is 8×10 4 Da, the molecular weight of PLGA is 5×10 4 Da;

[0033] Synthetic method: using stannous chloride (0.5%) as a catalyst, racemic lactic acid (dl-PLGA) and PCL are fed at a ratio of 1:1 to 1:2 (molar ratio), and dl-PLGA and PCL are mixed at 180 ℃, 70Pa under direct melt copolymerization for 12 hours, can obtain intrinsic viscosity poly(caprolactone-lactic acid glycolic acid), that is, the PCL-PLGA polymer of the present invention, its ...

Embodiment 2

[0037] 1) Preparation of spinning solution:

[0038]In parts by volume, 9 parts of trifluoroethanol and 1 part of distilled water are mixed to prepare a spinning solvent; the mixture of PCL-PLGA polymer and paclitaxel is added to the above spinning solvent and the concentration of the mixture in the spinning solvent is 10wt%; stirring at 25-30°C for 12 hours to fully dissolve the mixture; standing for defoaming for 2 hours to obtain a PCL-PLGA electrospinning solution;

[0039] Wherein, in the mixture, the amount of paclitaxel is 1wt% of the amount of the mixture; in the PCL-PLGA polymer, the molecular weight of PCL is 8×10 4 Da, the molecular weight of PLGA is 5×10 4 Da; synthetic method is the same as in Example 1, below.

[0040] 2) Preparation of nanofibers:

[0041] The PCL-PLGA electrospinning solution obtained in step 1) was subjected to electrospinning at a humidity of 30-50% and a temperature of 25-30°C. The spinning voltage was 8kV, and the flow rate of the spinni...

Embodiment 3

[0043] 1) Preparation of spinning solution:

[0044] In parts by volume, 9 parts of trifluoroethanol and 1 part of distilled water are mixed to prepare a spinning solvent; the mixture of PCL-PLGA polymer and paclitaxel is added to the above spinning solvent and the concentration of the mixture in the spinning solvent is 10wt%; stirring at 25-30°C for 12 hours to fully dissolve the mixture; standing for defoaming for 2 hours to obtain a PCL-PLGA electrospinning solution;

[0045] Wherein, in the mixture, the amount of paclitaxel is 2wt% of the amount of the mixture; in the PCL-PLGA polymer, the molecular weight of PCL is 8×10 4 Da, the molecular weight of PLGA is 5×10 4 Da;

[0046] 2) Preparation of nanofibers:

[0047] The PCL-PLGA electrospinning solution obtained in step 1) was subjected to electrospinning at a humidity of 30-50% and a temperature of 25-30°C. The spinning voltage was 8kV, and the flow rate of the spinning solution was 800 μL / h. The horizontal distance b...

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Abstract

The invention discloses a PCL-PLGA slow-release preparation and a preparation method thereof. The preparation method comprises the following steps: dissolving an antitumor medicine and a PCL-PLGA copolymer in a spinning solvent, stretching a spinning solution into micro / nanofiber under the action of a high-voltage electric field by an electrostatic spinning technology, and receiving the micro / nanofiber on the surface of a fixed receiver to obtain the PCL-PLGA slow-release preparation. The slow-release preparation provided by the invention gives full play to excellent biocompatibility and fat solubility of a PLGA material, further solves the problems of low mechanical toughness and too short degradation cycle through PCL-PLGA copolymerization, and has the advantages of capabilities of prolonging the circulation time of a chemotherapeutic medicine in a body, improving the blood concentration at a tumor site and reducing adverse effects of the chemotherapeutic medicine, and the like.

Description

technical field [0001] The invention belongs to the technical field of sustained-release preparations, and in particular relates to a PCL-PLGA sustained-release preparation and a preparation method thereof. Background technique [0002] Electrospinning is currently one of the most important ways to obtain continuous nanoscale and submicron polymer fibers. Because the fibers prepared by electrospinning technology have the characteristics of small diameter, large specific surface area, high porosity, strong adsorption and good spatial connectivity, they are widely used in the field of biomedicine as drug slow-controlled release carriers and tissue engineering scaffolds. , wound dressings, etc. Polymers have good biocompatibility and degradability in vivo, and the electrospun fiber drug loading with polymers as carriers provides a new idea for the development of sustained-release preparations, and has been widely used in the field of biomedicine. Taking PLGA as an example, it...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/34D01D5/00D04H1/4326D04H1/728A61P35/00A61K31/337A61K31/12A61K31/585
CPCA61K9/70A61K31/12A61K31/337A61K31/585A61K47/34D01D5/003D01D5/0076D01D5/0092D04H1/4326D04H1/728
Inventor 汤须崇寇馨月韦若帆
Owner HUAQIAO UNIVERSITY
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