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Camptothecine derivative phosphatide composite liposome nano-preparation and its making method

A technology of lipid nanoparticles and phospholipid complexes, applied in the field of medicine, can solve problems such as unsatisfactory dispersion effect, and achieve the effects of improving bioavailability, preventing hydrolysis and reducing dosage

Active Publication Date: 2007-09-05
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the dispersion effect of simple camptothecin derivative phospholipid complex in water is not very satisfactory, and a large proportion of phospholipid is required to prepare the complex, and the weight ratio of camptothecin to phospholipid is as high as 1:80-93
[0009] In summary, it can be seen that there is no clinically available drug preparation that maintains the active ring structure of camptothecin lactone and has a high drug loading capacity.

Method used

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  • Camptothecine derivative phosphatide composite liposome nano-preparation and its making method
  • Camptothecine derivative phosphatide composite liposome nano-preparation and its making method
  • Camptothecine derivative phosphatide composite liposome nano-preparation and its making method

Examples

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Embodiment 1

[0037] Get 10mg of 10-hydroxycamptothecin, dissolve it in 10ml of absolute ethanol at 50°C to obtain a blue fluorescent clear liquid, keep it warm at 50°C, add soybean lecithin (average molecular weight 780), stir until the solution is clear, after about 10min, connect the reflux device, keep at 50°C, stir for 2h, add 50ul of soybean oil for injection, continue stirring for 5min, remove the reflux device, evaporate the organic solvent to dryness under reduced pressure, add water for injection 10ml, stirred, and high-pressure milked 7 times to obtain hydroxycamptothecin phospholipid complex lipid nanoparticles. The particle diameter is 146nm, and the PDI is 0.146, see accompanying drawing 1.

Embodiment 2

[0039] Take 10mg of camptothecin, dissolve it in 10ml of acetone at 45°C to obtain a blue fluorescent clear liquid, keep it warm at 45°C, add soybean lecithin (average molecular weight 750) in an equal molar amount to camptothecin, and stir until the solution is clear After about 10 minutes, connect the reflux device, keep at 45°C, stir for 1.5 hours, add 100ul of medium-chain fatty acid ester, continue to stir for 5 minutes, remove the reflux device, evaporate the organic solvent under reduced pressure, add 10ml of water for injection, stir, and high-pressure milk Homogenize 5 times to obtain camptothecin-phospholipid complex lipid nanoparticles. The particle size is 155 nm, and the PDI is 0.167.

Embodiment 3

[0041] Take 10mg of 10-methoxycamptothecin, dissolve it in 10ml of acetone at 45°C to obtain a blue fluorescent clear liquid, keep it warm at 45°C, add egg yolk in an amount equivalent to 3 times the molar amount of 10-methoxycamptothecin Phospholipids (average molecular weight 800), stir until the solution is clear, after about 10 minutes, connect the reflux device, keep at 45°C, stir for 2 hours, add 100 mg of glyceryl monostearate, continue stirring for 10 minutes, remove the reflux device, and evaporate to dryness under reduced pressure Organic solvent, add 10ml of water for injection, stir, and high-pressure milk for 7 times to obtain solid lipid nanoparticles of 10-methoxycamptothecin phospholipid complex. The particle diameter is 173 nm, and the PDI is 0.228. Add 8% sucrose, reconstitute after lyophilization, the particle size is 178nm, and the PDI is 0.242.

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Abstract

A lipoid nanoparticle of camptothecine-phosphatide composition is prepared from phosphatide, 10-hydroxy camptothecine or its derivative and lipoid. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to the technical field of medicine, and specifically provides a camptothecin derivative phospholipid complex lipid nanoparticle preparation and a preparation method thereof that can be widely used in industrial production. Background technique [0002] Camptothecin (camptothecin, CPT) is an alkaloid antineoplastic drug extracted from the unique plant Camptotheca japonica in my country. It has strong biological activity, but its large adverse reactions limit its clinical application. The structural formula of camptothecin (CPT) is: [0003] [0004] Camptothecin drugs can be directly extracted from camptotheca or modified in structure. They are selective DNA topoisomerase inhibitors and have broad-spectrum anti-tumor effects. Both in vitro and animal experiments have shown that 10-hydroxycamptothecin (10-hydroxyl camptothecin, HCPT) has a stronger anti-tumor effect and a wider anti-tumor spectrum than CPT, and its toxicity is r...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4745A61P35/00
Inventor 张志荣龚涛卫薇
Owner SICHUAN UNIV
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