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Hydroxycamptothecin nano lipid bundle preparation and preparation method thereof

A technology of hydroxycamptothecin and lauryl hydroxystearate, which is applied in the field of 10-hydroxycamptothecin nano-lipid beam preparation and its preparation, to achieve uniform microemulsion particle size distribution, enhance active and passive targeting of tumors Integrating functions, the effect of simple formula and process

Active Publication Date: 2016-01-20
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, how to make the target drug, ie, hydroxycamptothecin, solubilizer, and reagents for surface PEGylation and targeting, into microemulsions has encountered great difficulties in practice.

Method used

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  • Hydroxycamptothecin nano lipid bundle preparation and preparation method thereof
  • Hydroxycamptothecin nano lipid bundle preparation and preparation method thereof
  • Hydroxycamptothecin nano lipid bundle preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0050] 1. Preparation of hydroxycamptothecin nano-resin bundle oil

[0051] 1. Weigh 0.8 g of phospholipid (Lipoid, Germany) and 0.8 g of propylene glycol and dissolve to obtain solution A.

[0052] 2. Weigh 0.025g of hydroxycamptothecin, 3.0g of ethanol, 3.8g of SolutolHS15 (BASF, Germany), 0.038g of folic acid-PEGDSPE, and 2.6g of glycerol, and dissolve at room temperature to obtain solution B.

[0053] 3. Mix solution A and solution B, stir and mix at room temperature to obtain a clear and transparent hydroxycamptothecin nano-fatty oil agent, which is protected by nitrogen and sealed.

[0054] 2. Preparation of hydroxycamptothecin nano-lipid bundle injection

[0055] The hydroxycamptothecin nanometer lipid bundle oil preparation prepared in the first step is diluted with 20 times the volume of physiological saline to obtain the hydroxycamptothecin nanometer injection.

[0056] 3. Determination of Microemulsion Particle Size of Hydroxycamptothecin Nano-Lipid Beam Injection...

preparation example 2

[0060] 1. Preparation of hydroxycamptothecin nano-resin bundle oil

[0061] 1. Weigh 0.9 g of phospholipid (Lipoid, Germany) and 3.0 g of ethanol, and dissolve to obtain solution A.

[0062] 2. Weigh 0.02 g of hydroxycamptothecin, 0.9 g of propylene glycol, 3.6 g of SolutolHS15 (BASF, Germany), 50 mg of cholic acid-PEGDSPE, and 1.6 g of glycerol, and dissolve to obtain solution B.

[0063] 3. Mix solution A and solution B, stir and mix at room temperature to obtain a clear and transparent hydroxycamptothecin nano-fatty oil agent, which is protected by nitrogen and sealed.

[0064] 2. Preparation of hydroxycamptothecin nano-lipid bundle injection

[0065] The hydroxycamptothecin nano lipid bundle oil preparation prepared in step 1 is diluted with 20 times the volume of physiological saline to obtain the hydroxycamptothecin nano lipid bundle injection, and the injection is an emulsion.

[0066] 3. Determination of Microemulsion Particle Size of Hydroxycamptothecin Nano Injecti...

preparation example 3

[0069] 1. Preparation of hydroxycamptothecin nano-resin bundle oil

[0070] 1. Weigh 1.0 g of phospholipid (Lipoid, Germany) and 1.0 g of propylene glycol and dissolve to obtain solution A.

[0071] 2. Weigh 0.025 g of hydroxycamptothecin, 3.6 g of ethanol, 3.8 g of SolutolHS15 (BASF, Germany), 60 mg of sialic acid-PEGDSPE, and 1.6 g of glycerol, and dissolve at room temperature to obtain solution B.

[0072] 3. Mix solution A and solution B, stir and mix at room temperature to obtain a clear and transparent hydroxycamptothecin nano-fatty oil agent, which is protected by nitrogen and sealed.

[0073] 2. Preparation of hydroxycamptothecin nano-lipid bundle injection

[0074] The hydroxycamptothecin nano lipid bundle oil preparation prepared in step 1 is diluted with 20 times the volume of physiological saline to obtain the hydroxycamptothecin nano lipid bundle injection, and the injection is an emulsion.

[0075] 3. Determination of Microemulsion Particle Size of Hydroxycampt...

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Abstract

The invention relates to hydroxycamptothecine lipid nanobundle oil and a hydroxycamptothecine lipid nanobundle injection which have an active targeting function, and preparation methods thereof. The hydroxycamptothecine lipid nanobundle oil comprises phospholipid, polyethylene glycol-12-hydroxystearate, glycerol, propylene glycol, ethanol and hydroxycamptothecine and X-PEG-DSPE (polyethylene glycol-distearoyl phosphatidyl ethanolamine), wherein the X-PEG-DSPE is selected from folic acid-PEG-DSPE, cholic acid-PEG-DSPE, CRGDK-PEG-DSPE, sialic acid-PEG-DSPE and oligose-PEG-DSPE. The hydroxycamptothecine lipid nanobundle oil is dissolved in water for injection to obtain the hydroxycamptothecine lipid nanobundle injection which is uniform in particle size, can reduce the toxicity of hydroxycamptothecine, has long-circulation effect and can enhance tumor targeting enrichment and improve patient compliance. The hydroxycamptothecine lipid nanobundle oil and hydroxycamptothecine lipid nanobundle injection are simple in preparation methods and can meet different needs of clinical applications.

Description

technical field [0001] The invention relates to the technical field of drug nano-lipid bundle preparations, in particular to a 10-hydroxycamptothecin nano-lipid bundle preparation with active targeting function and a preparation method thereof. Background technique [0002] As a cytotoxic alkaloid, camptothecin (CPT) was isolated from the plant Camptotheca in the 1950s. Binding to the topoisomerase 1-DNA complex can inhibit the religation step during the relaxation of DNA supercoiled structure, which in turn leads to apoptosis of tumor cells with high topoisomerase expression. Initial studies found that not only the side effects of hemorrhagic cystitis and bone marrow toxicity hindered the further application of camptothecin, but also its low water solubility greatly hindered its clinical application. [0003] Reducing toxicity, increasing solubility and improving efficacy are the development directions of camptothecin drugs. Through the structural modification of position...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K31/4745A61K9/08A61P35/00
Inventor 梁兴杰赵元元陈飞马晓溦李盛亮薛向东柳娟金叔斌李鸿基张吉梅王义峰甘雅玲姜永刚
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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