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Lipid body loaded with chloroquine drugs and paclitaxel drugs together and preparation method of same

A paclitaxel and chloroquine technology is applied in the field of co-loaded liposomes of chloroquine drugs and paclitaxel drugs and their preparation, which can solve the problems of poor, drug resistance and anti-cancer effects of cells, and achieves reduction in usage, overcoming Multidrug resistance, the effect of increasing lethality

Active Publication Date: 2012-12-26
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, paclitaxel preparations that have been approved for clinical use or are undergoing clinical evaluation are mainly liposome preparations, such as paclitaxel liposome for injection, trade name Lipusu, although it avoids the effects of allergic reactions caused by solvents and drug interactions. , but there is still the problem that it is easy to make cells develop drug resistance, so that the anti-cancer effect is not good

Method used

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  • Lipid body loaded with chloroquine drugs and paclitaxel drugs together and preparation method of same
  • Lipid body loaded with chloroquine drugs and paclitaxel drugs together and preparation method of same

Examples

Experimental program
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Embodiment 1

[0036] Weigh 250mg of soybean phospholipids (phosphatidylcholine purity> 76%) and 50mg of cholesterol were dissolved in 3mL of absolute ethanol, and then 2mg of paclitaxel dissolved in 2ml of absolute ethanol was added. After fully dissolving, the mixture was mixed uniformly, and then the organic solvent ethanol was evaporated under reduced pressure, so that the film-forming materials such as phospholipids were on the bottom of the flask. A uniform lipid film is formed, then 2mL PBS (phosphate, pH=7.4) buffer is added, vortexed for 5 minutes, and finally sonicated with a cell pulverizer for 5 minutes to obtain 2ml of paclitaxel liposome suspension, which is measured The average particle size (number average) is 98.6nm. Sephadex G-50 gel column chromatography is used to separate liposomes and unencapsulated free drugs. The encapsulation rate of paclitaxel is 99.65%, and the drug loading is 0.66%.

Embodiment 2

[0038] Weigh 250mg of soybean phospholipids (phosphatidylcholine purity> 76%) and 50mg of cholesterol were dissolved in 3mL of absolute ethanol, and then 2mg of paclitaxel dissolved in 2ml of absolute ethanol was added. After fully dissolving, the mixture was mixed uniformly, and then the organic solvent ethanol was evaporated under reduced pressure, so that the film-forming materials such as phospholipids were on the bottom of the flask. A uniform lipid film is formed, and then 2mL 0.3mol / L citric acid-sodium citrate buffer solution (pH=3.5) is added, vortexed for 5 minutes, and finally sonicated with a cell pulverizer for 5 minutes to obtain 2ml of paclitaxel liposome suspension for use.

Embodiment 3

[0040] Weigh 210mg dipalmitoylphosphatidylcholine (DPPC), 40mg phosphatidylethanolamine (PE) and 50mg cholesterol, dissolve them in 3mL absolute ethanol, add 2mg paclitaxel dissolved in 2ml absolute ethanol, fully dissolve and mix well. Then, the organic solvent ethanol was evaporated under reduced pressure to make the membrane-forming materials such as phospholipids form a uniform lipid film on the bottom of the flask. Then, 2mL PBS (phosphate, pH=7.4) buffer was added, vortexed for 5 minutes, and finally sonicated with a cell pulverizer for 5 minutes. Obtain 2ml of paclitaxel liposome suspension. The average particle size of the liposome suspension was measured to be 102nm. Sephadex G-50 gel column chromatography was used to separate liposomes and unencapsulated free drug. Paclitaxel The encapsulation rate is 100%, and the drug loading is 0.66%.

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Abstract

The invention discloses a lipid body loaded with chloroquine drugs and paclitaxel drugs together. The lipid body comprises drugs, phosphatide, cholesterin compounds, an internal buffering system and pH value conditioning agents, wherein, the mass ratio of the drugs, the phosphatide and the cholesterin compounds is 1:2 to 125:1 to 45; and the drugs are the chloroquine drugs and the paclitaxel drugs. Due to the chloroquine drugs and the paclitaxel drugs, the lipid body loaded with chloroquine drugs and the paclitaxel drugs together is characterized in that multidrug resistance can be inhibited, and the drug toxicity can be reduced. The invention further discloses a preparation method of the lipid body loaded with chloroquine drugs and the paclitaxel drugs together; in addition, the preparation technology is simple, the condition is mild, controlling parameters are less, and the preparation method facilitates to lower the manufacturing cost and achieves easy industrialized production.

Description

Technical field [0001] The invention relates to the technical field of liposome drugs, in particular to a liposome co-loaded with chloroquine drugs and paclitaxel drugs and a preparation method thereof. Background technique [0002] Tumor is one of the main diseases threatening human health. Chemotherapeutic drugs are the main means of treatment. However, due to the massive use of chemotherapeutics, tumor cells are prone to multidrug resistance (MDR), and the generation of MDR is currently One of the main reasons for the failure of tumor chemotherapy. [0003] Paclitaxel (Tax) is an alkaloid with a unique anti-cancer mechanism and has certain effects on the treatment of various advanced cancers. However, due to its extremely low solubility in water, it cannot be absorbed by oral administration. The Tax injection currently used in clinical practice is a concentrated solution made of polyoxyethylene castor oil / absolute ethanol mixed solvent. It must be diluted before use, which is n...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4706A61K9/127A61P35/00A61K31/337
Inventor 邱利焱高梦华
Owner ZHEJIANG UNIV