Preparation and application of anti-tumor activator nanostructure lipid carrier

A nano-structured lipid and surfactant technology, applied in the field of biomedicine, can solve the problems of limitation, poor water solubility, and unstable metabolism, and achieve good anti-tumor effects and improve poor solubility.

Inactive Publication Date: 2013-08-28
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the unstable metabolism of the drug in the organism

Method used

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  • Preparation and application of anti-tumor activator nanostructure lipid carrier
  • Preparation and application of anti-tumor activator nanostructure lipid carrier
  • Preparation and application of anti-tumor activator nanostructure lipid carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1: Preparation of Blank Nanostructured Lipid Carrier

[0076] Weigh 0.333g glyceryl monostearate and 0.666g caprylic acid / capric triglyceride in a 100ml eggplant-shaped bottle with an analytical balance, heat in a water bath, and keep the temperature at 60°C. Weigh 0.4g Tween 80 and stir to disperse in PBS buffer (PH7.4) (preparation method: 8gNaCl+0.2gKCl+2.94gNa 2 HPO 4 12H 2 O+0.2g ​​KH 2 PO 4 , distilled water to 1000ml). After the solid-liquid phase lipid is melted, under stirring, the PBS buffer solution dispersed with Tween 80 is added dropwise into the molten solid-liquid lipid, and the stirring is continued to obtain a pre-emulsion, and the volume is constant. The pre-emulsion is subjected to probe ultrasonication, and the probe is ultrasonically cooled to room temperature to form a nanostructured lipid carrier water dispersion system.

Embodiment 2

[0077]Example 2: Preparation of 17-propenylamino-17-desmethoxygeldanamycin nanostructured lipid carrier

[0078] Weigh 0.333g of glyceryl monostearate and 0.666g of caprylic / capric triglyceride in a 100ml eggplant-shaped bottle with an analytical balance, heat in a water bath, and keep the temperature at 60°C. After the solid-liquid phase lipids are melted, stir 1 ml of 17-AAG ethanol solution with a concentration of 2 mg / ml was added dropwise. Weigh 0.4g Tween 80 and stir to disperse in PBS buffer (PH7.4) (preparation method: 8gNaCl+0.2gKCl+2.94gNa 2 HPO 4 12H 2 O+0.2gKH 2 PO 4 , distilled water to 1000ml). Under stirring, the PBS buffer solution that will be dispersed with Tween 80 is added dropwise in the solid-liquid lipid of melting, continues stirring to obtain pre-emulsion, constant volume. The pre-emulsion is subjected to probe ultrasonication, and the probe is ultrasonically cooled to room temperature to form a nanostructured lipid carrier water dispersion syste...

Embodiment 3

[0080] Blank nanostructured lipid carrier, the ratio of each component is as follows:

[0081] The sum of solid phase lipid and liquid phase lipid is 5% (W / V),

[0082] The ratio of solid phase lipids to liquid phase lipids, the mass ratio is: 1:0.5,

[0083] The content of surfactant is 1% (W / V),

[0084] The rest are solvents for injection.

[0085] Among them, the ratio of solid phase lipid and liquid phase lipid is 1:0.5. Wherein the solid phase lipid is preferably glyceryl monostearate, and the liquid phase lipid is caprylic acid / capric triglyceride.

[0086] Wherein said surfactant is preferably Tween 80.

[0087] Wherein the solvent for injection is originally selected from: water for injection, physiological saline, and isotonic PBS buffer solution of pH 7.4.

[0088] The preparation method of the blank nanostructured lipid carrier of the present invention is as follows: Weigh the solid-phase lipid and liquid-phase lipid, mix the above-mentioned components uniform...

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Abstract

The invention relates to a preparation and application of an anti-tumor activator nanostructure lipid carrier, and in particular relates to a 17-allylamino-17-demethoxygeldanamycin nanostructure lipid carrier which has the following formula: 50 to 500mg/L of medicament, 50 to 150g/L of nanostructure lipid carrier taking medium chain triglyceride as a liquid-phase lipid, 10 to 30g/L of surfactant and the balance of solvent for injection.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a new dosage form of an antitumor active agent, in particular to a 17-propenylamino-17-desmethoxygeldanamycin nanostructured lipid carrier and a preparation method. The invention also relates to the application of the nanostructured lipid carrier in enhancing the drug effect and sustained release effect of the anti-tumor active agent and changing the pharmacokinetics of the drug in vivo. Background technique [0002] Lipid nanoparticles are a new type of drug nanocarrier developed in the 1990s. They use biocompatible lipid materials as carriers to dissolve or wrap drugs or other biologically active substances in lipid cores or adsorb them. , a novel drug-loading system attached to the surface of nanoparticles. [0003] Nanostructured lipid carriers (NLC) are developed from solid lipid nanoparticles (SLN). It is a lipid nanoparticle delivery carrier prepared by mixing solid lipids and st...

Claims

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Application Information

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IPC IPC(8): A61K47/14A61K31/395A61K9/16A61P35/00
Inventor 崔国辉崔纯莹刘小征
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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