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Composition for treating intervertebral disc degeneration diseases, liposome nano drug delivery system and preparation method and application of liposome nano drug delivery system

A technology for degenerative diseases and drug delivery systems, applied in the field of medicine, can solve the problems of large dosage, low bioavailability, difficulty in finding a solvent solubility requirement, etc., and achieves convenient administration, improved compliance, small amount and high efficiency passive. targeted effect

Inactive Publication Date: 2020-10-23
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Since oleanolic acid is a fat-soluble component and icariin is a water-soluble component, it is difficult to find a suitable solvent to meet the solubility requirements of the two at the time of injection administration; such as preparing them into tablets, capsules, etc. Solid preparations have low bioavailability and high dosage when administered orally; therefore, there is no relevant report on the combination of oleanolic acid and icariin for the treatment of intervertebral disc degenerative diseases

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: the preparation of the liposome nano drug delivery system of the composition for the treatment of intervertebral disc degenerative disease

[0025] In this embodiment, the mass ratio of oleanolic acid to icariin is 1:10, the mass ratio of oleanolic acid to distearoylphosphatidylcholine is 1:5, and the surfactant TPGS and distearoyl The mass ratio of phosphatidylcholine is 1:8, and the mass ratio of cholesterol and distearoylphosphatidylcholine is 1:1;

[0026] Oleanolic acid, surfactant TPGS, cholesterol and distearoylphosphatidylcholine were dissolved in chloroform / ethanol solution, then rotary evaporation under reduced pressure to remove organic reagents to obtain an organic phase; icariin Dissolve in 3ml of phosphate-buffered saline buffer solution (pH6.5, concentration 10mmol / ml), add the organic phase, stir in a water bath at 60°C for 30 minutes, sonicate for 2 minutes with an ultrasonic cell pulverizer, pass through a 0.22μm filter membrane to obtain...

Embodiment 2

[0027] Embodiment 2: the preparation of the liposome nano drug delivery system of the composition for the treatment of intervertebral disc degenerative disease

[0028] In this embodiment, the mass ratio of oleanolic acid to icariin is 1:1, the mass ratio of oleanolic acid to soybean lecithin is 1:17.5, the mass ratio of surfactant TPGS to soybean lecithin is 1:29, and the mass ratio of cholesterol The mass ratio to soybean lecithin is 1:10;

[0029] Dissolve oleanolic acid, surfactant TPGS, cholesterol and soybean lecithin in chloroform / ethanol solution, then evaporate under reduced pressure to remove organic reagents to obtain an organic phase; dissolve icariin in 3ml of phosphate buffered saline Add the organic phase to the solution buffer (pH6.5, concentration 10mmol / ml), stir in a water bath at 60°C for 45 minutes, sonicate with an ultrasonic cell pulverizer for 4 minutes, and pass through a 0.22 μm filter membrane to obtain the liposome nanometer Drug system, the prepar...

Embodiment 3

[0030] Embodiment 3: the preparation of the liposome nano drug delivery system of the composition for the treatment of intervertebral disc degenerative disease

[0031] In this embodiment, the mass ratio of oleanolic acid to icariin is 10:1, the mass ratio of oleanolic acid to dipalmitoylphosphatidylcholine is 1:30, and the surfactant TPGS and dipalmitoylphosphatidylcholine The mass ratio of choline is 1:50, and the mass ratio of cholesterol and dipalmitoylphosphatidylcholine is 1:20;

[0032]Dissolve oleanolic acid, surfactant TPGS, cholesterol and dipalmitoylphosphatidylcholine in chloroform / ethanol solution, and then rotary evaporate under reduced pressure to remove organic reagents to obtain an organic phase; dissolve icariin In 3ml of phosphate-buffered saline buffer (pH6.5, concentration 10mmol / ml), add the organic phase, stir in a water bath at 60°C for 1 hour, sonicate for 6 minutes with an ultrasonic cell pulverizer, and pass through a 0.22 μm filter membrane to obtai...

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Abstract

The invention discloses a composition for treating intervertebral disc degeneration diseases, a liposome nano drug delivery system and a preparation method and application of the liposome nano drug delivery system. The composition consists of oleanolic acid and icariin according to the mass ratio of 1:10 to 10:1. The liposome nano drug delivery system is a nano liposome preparation prepared from the composition, a surfactant TPGS, cholesterol and phospholipid. The composition composed of oleanolic acid and icariin provided by the invention has the effects of benefiting qi, dispersing blood stasis and tonifying kidney, and can be used for preparing drugs for treating intervertebral disc degeneratipm diseases; particularly, the liposome nano drug delivery system of the composition provided by the invention can effectively improve the bioavailability of oleanolic acid and icariin in the composition and reduce the taking dosage and toxicity of the composition, is convenient to take, smallin dosage and efficient, has a certain passive targeting property, improves the compliance of patients, and has popularization and application values.

Description

technical field [0001] The invention relates to a composition for treating intervertebral disc degenerative diseases, a liposome nano drug delivery system, a preparation method and application thereof, and belongs to the technical field of medicine. Background technique [0002] Intervertebral disc degeneration (IVDD) is an aging disease characterized by loss of extracellular matrix. According to the article "The Initiating Factors, Intermediate Links and Outcomes of Intervertebral Disc Degeneration" published by Wang Yongjun and other researchers in the "Chinese Journal of Orthopedics and Traumatology" No. 3, 2000, it can be seen that affected by the congenital structure of poor blood supply, the cartilage endplate pathway and peripheral pathways of the annulus fibrosus can provide limited nutrition. With age, cellular senescence, genetic phenotype changes, increased metabolic capacity, and extracellular matrix disturbances further exacerbate IVDD. Intervertebral disc her...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K31/7048A61K9/127A61P19/08
CPCA61K9/127A61K31/56A61K31/7048A61K47/28A61P19/08A61K2300/00
Inventor 查建林李晨光
Owner SHANGHAI UNIV OF T C M