Solid liposome nano granule with antineoplastic activity

A technology of solid lipid nanoparticles and anti-tumor activity, which is applied in the field of solid lipid nanoparticles with anti-tumor activity to achieve the effects of reducing distribution, improving curative effect and increasing uptake

Inactive Publication Date: 2007-08-08
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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But can cause a variety of adverse reactions including severe allergic reactions

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  • Solid liposome nano granule with antineoplastic activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1: Preparation and application of monoglyceride solid lipid nanoparticles loaded with paclitaxel

[0013] 1) Preparation of paclitaxel monoglyceride solid lipid nanoparticles

[0014] Accurately weigh 30 mg of monoglycerides and 1.5 mg of paclitaxel, place them in 3 mL of absolute ethanol, and dissolve them in a water bath at 70°C. Use distilled water as the dispersed phase and place it in a 70°C water bath. At 400r·min -1 Under mechanical stirring conditions, the organic phase was poured into 30 mL of the dispersed phase and stirred for 5 minutes to obtain a dispersion of solid lipid nanoparticles loaded with paclitaxel monoglyceride. The obtained solid lipid nanoparticle dispersion loaded with paclitaxel monoglyceride used 3mol·L -1 Adjust the pH to 1.2 with HCl solution at 20000r·min -1 Centrifuge for 10 minutes, add 0.1% Poloxamer (w / v) to the precipitate and disperse again, then use 1mol·L -1 Adjust the pH to 7.0 with NaOH solution. The solid lipid nanoparticle...

Embodiment 2

[0026] Example 2: Preparation and application of stearic acid solid lipid nanoparticles loaded with paclitaxel

[0027] 1) Preparation of Paclitaxel Stearic Acid Solid Lipid Nanoparticles

[0028] Accurately weigh 30 mg stearic acid and 1.5 mg paclitaxel, place them in 3 mL absolute ethanol, and dissolve them in a water bath at 70°C. Use distilled water as the dispersed phase and place it in a 70°C water bath. At 400r·min -1 Under mechanical stirring conditions, the organic phase was poured into 30 mL of the dispersed phase and stirred for 5 minutes to obtain a dispersion of solid lipid nanoparticles loaded with paclitaxel stearic acid. The obtained dispersion of solid lipid nanoparticles loaded with paclitaxel stearic acid used 3mol·L -1 Adjust the pH to 1.2 with HCl solution at 20000r·min -1 Centrifuge for 10 minutes, add 0.1% Poloxamer (w / v) to the precipitate and disperse again, then use 1mol·L -1 Adjust the pH to 7.0 with NaOH solution. The solid lipid nanoparticles loaded with...

Embodiment 3

[0033] Example 3: Preparation and application of paclitaxel-loaded glyceryl tristearate solid lipid nanoparticles

[0034] 1) Preparation of Paclitaxel Tristearate Solid Lipid Nanoparticles

[0035] Accurately weigh 30 mg stearic acid and 1.5 mg paclitaxel, place them in 3 mL absolute ethanol, and dissolve them in a water bath at 70°C. Use distilled water as the dispersed phase and place it in a 70°C water bath. At 400r·min -1 Under mechanical stirring conditions, the organic phase was poured into 30 mL of the dispersed phase and stirred for 5 minutes to obtain a dispersion of solid lipid nanoparticles loaded with paclitaxel tristearate. The obtained solid lipid nanoparticle dispersion loaded with paclitaxel tristearate is used 3mol·L -1 Adjust the pH to 1.2 with HCl solution at 20000r·min -1 Centrifuge for 10 minutes, add 0.1% Poloxamer (w / v) to the precipitate and disperse again, then use 1mol·L -1 Adjust the pH to 7.0 with NaOH solution. The solid lipid nanoparticles loaded wit...

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Abstract

The invention relates to a nanometer liposome carrier with high-effect anti-tumor activity, which carries the anti-tumor Paclitaxel, while the Paclitaxel is 3.1-3.6% of solid liposome nanometer particles, and the diameter is 481-532nm. The invention has high-effect cell extraction and cell-pulp hold function via the nanometer liposome carrier, while the package on the anti-tumor drug whose molecule target is at the cell pulp can improve the adsorption of anti-tumor drug and improve the drug density at target part. The invention can improve the drug adsorption of tumor cell, reduce the drug distribution at normal cell, reduce the side effect and toxicity, and improve the effect.

Description

Technical field [0001] The invention relates to the preparation of solid lipid nanoparticles loaded with anti-tumor drugs and the application of the drug delivery system in anti-tumor treatment. Background technique [0002] Tumor has always been a major disease that directly threatens human health. Due to the lack of molecular targeting of the drug itself, tumor chemotherapy has major treatment problems such as low cure rate and huge side effects. Through appropriate carrier technology, direct targeting of drugs to diseased tissues (organs), cells and subcellular organelles is one of the important means to solve the low cure rate and toxic side effects of cancer chemotherapy. At present, scientists at home and abroad have made certain progress in the tissue (organ) and cell targeting of tumor drugs through carrier technology, but they have not achieved breakthrough curative effects. The essence is that the molecular targets of most anti-tumor drugs are located in cells. Therefor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/12A61K47/14A61K31/337A61P35/00
Inventor 胡富强杜永忠袁弘游剑
Owner ZHEJIANG UNIV
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