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Preparation method of medicine-carrying temperature-sensitive self-assembly lipidosome

A liposome and self-assembly technology, applied in directions such as liposome delivery, can solve problems such as low liposome encapsulation rate, and achieve the effects of simple method, safe operation and good application prospect.

Inactive Publication Date: 2013-07-24
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Liposomes obtained by traditional methods have high encapsulation efficiency and stability; while for amphiphilic drugs, such as some weak acids and weak bases, the oil-water partition coefficient is greatly affected by the pH and ionic strength of the medium, and the prepared lipids Low body encapsulation efficiency

Method used

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  • Preparation method of medicine-carrying temperature-sensitive self-assembly lipidosome
  • Preparation method of medicine-carrying temperature-sensitive self-assembly lipidosome
  • Preparation method of medicine-carrying temperature-sensitive self-assembly lipidosome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Take by weighing the phosphatidylcholine of 0.05g, be dissolved in 5ml chloroform, add the ketoprofen of 0.5g poly-N-isopropylacrylamide and 0.006g, stir at room temperature on the magnetic stirrer, get containing medicine temperature. Sensitive polymer electrospray stock solution.

[0029] The prepared electrospray stock solution was introduced into the applicator (5mL syringe), and the No. 9 injection needle was used as the injection tube, connected to the positive electrode of the high-voltage power supply, and the aluminum foil microsphere receiving plate was connected to the negative electrode. The electrostatic spray process conditions are: voltage 10kv, flow rate 1.5mL / h, receiving plate distance 25cm, temperature 15°C, and air humidity 45%. The drug-loaded thermosensitive polymer microspheres were obtained. The observation picture of the polymer microspheres under the electron microscope is as follows: figure 1 shown.

Embodiment 2

[0031] Weigh 0.1g of phosphatidylcholine, dissolve it in 5ml of ethanol and chloroform (ethanol: chloroform = 1:1), add 0.5g of poly-N-isopropylacrylamide and 0.02g of ketoprofen, Stir at room temperature on a magnetic stirrer to obtain a temperature-sensitive polymer electrospray stock solution.

[0032] Introduce the prepared electrospray stock solution into the dosing device (5ml syringe), use a No. 9 injection needle as the injection tube, connect the positive electrode of the high-voltage power supply, and connect the aluminum foil microsphere receiving plate to the negative electrode. The electrostatic spray process conditions are: voltage 12kv, flow rate 1.0mL / h, receiving plate distance 20cm, temperature 25°C, and air humidity 80%. Acquired thermosensitive polymer microspheres. After vacuum drying, 2ml of high-purity water was added dropwise, evaporated to dryness naturally at 36°C, and observed with a transmission electron microscope, the results were as follows: f...

Embodiment 3

[0034] Weigh 0.2g of phosphatidylcholine, dissolve it in 10ml of ethanol and chloroform (ethanol: chloroform = 6:4), add 1g of poly-N-isopropylacrylamide and 0.08g of ketoprofen, and Stir on a stirrer at room temperature to obtain a temperature-sensitive polymer electrospray stock solution.

[0035] Introduce the prepared electrospray stock solution into the dosing device (5ml syringe), use a No. 9 injection needle as the injection tube, connect the positive electrode of the high-voltage power supply, and connect the aluminum foil microsphere receiving plate to the negative electrode. The electrostatic spray process conditions are: voltage 18kv, flow rate 0.5mL / h, receiving plate distance 10cm, temperature 20°C, and air humidity 57%. Acquired thermosensitive polymer microspheres. After vacuum drying, 10ml of high-purity water was added dropwise, evaporated to dryness naturally at 40°C, and observed with a transmission electron microscope, the results were as follows: image ...

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Abstract

The invention relates to a preparation method of medicine-carrying temperature-sensitive self-assembly lipidosome. The method comprises the following steps of: dissolving medicine-carrying temperature-sensitive macromolecules and lipidosome into an organic solvent, mixing and stirring; adding a lyophobic medicine to obtain a medicine-containing electronic injection stock solution; performing electrostatic spraying on the medicine-containing electronic injection stock solution; drying in vacuum and dropwise adding high-pure water; and drying by distillation to obtain the medicine-carrying temperature-sensitive self-assembly lipidosome. The lipidosome is practically applied to controlled release of the medicine; and the method is simple, rapid, safe to operate and suitable for large-scale production, and has good application prospect.

Description

technical field [0001] The invention belongs to the field of preparation of temperature-sensitive materials, in particular to a method for preparing drug-loaded temperature-sensitive self-assembled liposomes. Background technique [0002] As a drug carrier, liposome has the characteristics of improving drug efficacy, reducing adverse drug reactions and targeting effects. The commonly used preparation methods mainly include film dispersion method, reverse phase evaporation method, injection method, ultrasonic dispersion method, etc. Liposomes obtained by traditional methods have high encapsulation efficiency and stability; while for amphiphilic drugs, such as some weak acids and weak bases, the oil-water partition coefficient is greatly affected by the pH and ionic strength of the medium, and the prepared lipids The body encapsulation efficiency is low. [0003] Electrostatic spraying, as a new method of preparing microspheres, has attracted widespread attention in recent ye...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/192
Inventor 朱利民金成成权静石萌
Owner DONGHUA UNIV