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Preparation method of IMB16-4 liposome nanoparticles and medicine

A nanoparticle and liposome technology, which is applied in the direction of drug combinations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as poor patient compliance, low bioavailability, and inability to deliver drugs , to reduce toxic and side effects, improve solubility and absorption, and improve curative effect

Active Publication Date: 2022-07-22
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the solubility of IMB16-4 in water is low (approximately 40ng / ml), the bioavailability of conventional administration is low, and the drug cannot be delivered to the liver in sufficient concentration
Therefore, a large dosage is usually required to be effective, or IMB16-4 is administered after dissolving it in an organic solvent, but long-term large-dose administration has risks such as high drug cost, poor patient compliance, and potential side effects; and Many organic solvents cannot be used for human drug administration, even organic solvents such as ethanol that are less toxic and can be used for human body are not allowed to be used in large doses for a long time

Method used

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  • Preparation method of IMB16-4 liposome nanoparticles and medicine
  • Preparation method of IMB16-4 liposome nanoparticles and medicine
  • Preparation method of IMB16-4 liposome nanoparticles and medicine

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preparation example Construction

[0040] A preparation method of IMB16-4 liposome nanoparticle, such as figure 2 As shown, the preparation method includes:

[0041] Step 101: After dissolving IMB16-4 in the first organic solvent, add it to the first solution of polyvinylpyrrolidone (eg PVP K30), and stir to obtain the first nanosuspension. The first organic solvent includes, but is not limited to, dimethylformamide (DMF) or dimethylformamide (DMSO). Polyvinylpyrrolidone was used as a stabilizer to attach to the surface of IMB16-4 nanoparticles to stabilize them.

[0042] Step 102: After centrifuging the first nanosuspension, take a precipitate.

[0043]Step 103 : in the precipitation, add a second solution of polyvinylpyrrolidone for dispersion to obtain a second nanosuspension containing IMB16-4 nanoparticles, and perform step 104 or 105 . Wherein, the first solution or the second solution is a 0.1-0.5% w / v polyvinylpyrrolidone (eg PVP K30) aqueous solution. PVP K17, K12, etc. can also be used for polyvi...

Embodiment 1

[0058] Screening of the second organic solvent:

[0059] image 3 The preparation process of liposome nanoparticles is shown:

[0060] Step 301: Preparation of IMB16-4 nanoparticles: Dissolve 10 mg of IMB16-4 in 1 mL of DMF, and after complete dissolution, add dropwise to 10 mL of 0.1% w / v PVP K30 solution while magnetically stirring to obtain the first nano-mixture. suspension. Centrifuge the first nanosuspension, discard the supernatant, and take the pellet. 10 mL of 0.1% w / v PVP K30 was added to the precipitate for dispersion, and a nanosuspension with pale blue opalescence, namely the second nanosuspension, was obtained.

[0061] Step 302: Preparation of lipid film: Dissolve 15 mg of egg yolk lecithin and 3 mg of cholesterol in 6 mL of a second organic solvent, remove the second organic solvent by rotary evaporation, and obtain a lipid film at the bottom of the container.

[0062] Step 303: Preparation of IMB16-4 liposome nanoparticles: add the second nanosuspension (I...

Embodiment 2

[0070] Screening of phospholipid components:

[0071] Step 401: Preparation of IMB16-4 nanoparticles: Dissolve 10 mg of IMB16-4 in 1 mL of DMF, and after complete dissolution, add dropwise to 10 mL of 0.1% w / v PVP K30 solution while magnetically stirring to obtain the first nano-mixture. suspension. Centrifuge the first nanosuspension, discard the supernatant, and take the pellet. 10 mL of 0.1% w / v PVP K30 was added to the precipitate for dispersion, and a nanosuspension with pale blue opalescence, namely the second nanosuspension, was obtained.

[0072] Step 402: Preparation of lipid film: Dissolve phospholipid, DOTAP and cholesterol in 6 mL of n-butanol, remove the organic solvent by rotary evaporation, and obtain a lipid film at the bottom of the container.

[0073] Step 403: Preparation of IMB16-4 liposome nanoparticles: add the second nanosuspension (IMB16-4 nanoparticle concentration: 0.5 mg / mL) obtained in step 401 to the lipid film in step 402, at room temperature H...

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Abstract

The invention discloses a preparation method of I MB16-4 lipidosome nanoparticles and a medicine, and belongs to the technical field of pharmaceutical preparations, the preparation method comprises the following steps: dissolving I MB16-4 in a first organic solvent, then adding into a first solution of polyvinylpyrrolidone, and stirring to obtain a first nano suspension; after the first nano suspension is centrifuged, sediment is taken; adding a second solution of polyvinylpyrrolidone into the precipitate, and dispersing to obtain a second nano suspension; adding the second nano suspension into a lipid membrane to obtain a third nano suspension; hydrating the third nano suspension, and performing ultrasonic treatment to obtain a fourth nano suspension; and adding a freeze-drying protective additive into the fourth nano suspension, and carrying out freeze-drying, so as to obtain I MB16-4 liposome nanoparticle freeze-dried powder. The I MB16-4 is prepared into the liposome nanoparticles, so that the solubility and the absorption amount of the I MB16-4 are improved, the generation of MMP2, alpha-SMA and TGF-beta in liver cells is reduced, the anti-hepatic fibrosis curative effect is improved, and the toxic and side effects are reduced.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a preparation method and medicine of IMB16-4 liposome nanoparticle. Background technique [0002] The occurrence of liver fibrosis is related to chronic liver injury, and it is the protective wound repair response of the liver to various liver injuries. Liver fibrosis is the common pathological basis of various chronic liver diseases (CLDs), such as viral hepatitis, alcoholic hepatitis, non-alcoholic fatty liver, cholestatic hepatitis, autoimmune liver disease, etc. A critical step in the progression of CLDs to cirrhosis. Early liver fibrosis is reversible with appropriate treatment. However, if it develops further, the cellular response will be dysregulated, the extracellular matrix (ECM) will be excessively generated and degraded, resulting in excessive deposition of ECM, resulting in the destruction of the hepatic lobular structure, the disappearance of t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/63A61K47/24A61K9/19A61K9/10A61P1/16
CPCA61K31/63A61K9/5123A61K9/19A61K9/10A61P1/16
Inventor 牛霞李桂玲王玉成蒙亚楠牛冰羽王晓梅常格刘志锋
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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