Albumin-combined taxol long-circulation nano-particle freeze-dried preparation

An albumin-bound, freeze-dried preparation technology, applied in the field of medicine, can solve the problems of great physiological and psychological impact on patients with toxic side effects, long infusion time, etc., and achieve the effect of improving tumor targeting and reducing toxic and side effects

Inactive Publication Date: 2014-12-17
ACADEMY OF MILITARY MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to avoid allergic reactions, take dexamethasone 12 hours and 6 hours before the administration, and inject diphenhydramine orally and cetirizine 30 to 60 minutes before the administration, and slowly instill during the injection. Note time is longer
The toxic and side effects it brings have a great impact on the patient's physiology and psychology

Method used

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  • Albumin-combined taxol long-circulation nano-particle freeze-dried preparation
  • Albumin-combined taxol long-circulation nano-particle freeze-dried preparation
  • Albumin-combined taxol long-circulation nano-particle freeze-dried preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1. Blank albumin-bound long-circulation nanoparticles

[0026] Dissolve 300mg of human serum albumin in 30ml of water, then add 150mg of poloxamer 188 and slowly stir to dissolve, add 1ml of chloroform to shake, let it stand, separate the chloroform, repeat 3 times, so that the albumin aqueous solution is saturated with chloroform; take 0.55 1 ml and 0.05 ml of absolute ethanol were mixed, and dropped into the albumin aqueous solution drop by drop, stirred with a high-speed disperser, stirred for 10 seconds and then separated for 2 seconds, for a total of 2 minutes, to form colostrum; moved to a high-pressure homogenizer for high-pressure milk Mix well, and circulate 5 times at 3000psi to obtain nanoemulsion; the nanoemulsion uses a rotary evaporator to volatilize the organic solvent below 37°C, and the obtained suspension is translucent, transferred to a 5ml vial, 1ml / branch, and added 1ml of 20% mannitol, mixed evenly, is the blank albumin-bound long-circulati...

Embodiment 2

[0027] Example 2. Albumin-bound Paclitaxel Nanoparticles

[0028]Dissolve 300mg of human serum albumin in 30ml of water, add 1ml of chloroform to shake, let stand, separate the chloroform, repeat 3 times to make the albumin aqueous solution saturated with chloroform; mix 0.55ml of chloroform with 0.05ml of absolute ethanol, dissolve 50mg of paclitaxel , and drip into the albumin aqueous solution drop by drop, stir with a high-speed disperser, stir for 10 seconds and then 2 seconds apart, a total of 2 minutes, to form colostrum; move to a high-pressure homogenizer for high-pressure milk homogenization, and cycle 5 times at 3000psi , to get nanoemulsion; the nanoemulsion uses a rotary evaporator to volatilize the organic solvent below 37°C, and the obtained suspension is translucent, and is transferred to a 5ml vial, 1ml / support, and 1ml20% mannitol is added in addition, and mixed , namely albumin-bound paclitaxel nanoparticles.

Embodiment 3

[0029] Example 3. Lyophilized formulation of albumin-bound paclitaxel long-circulation nanoparticles

[0030] Dissolve 300mg of human serum albumin in 30ml of water, then add 150mg of poloxamer 188 and slowly stir to dissolve, add 1ml of chloroform to shake, let it stand, separate the chloroform, repeat 3 times, so that the albumin aqueous solution is saturated with chloroform; take 0.55 ml and 0.05ml of absolute ethanol were mixed to dissolve 50mg of paclitaxel, and dropwise added to the albumin aqueous solution, stirred with a high-speed disperser, stirring for 10 seconds and then at intervals of 2 seconds for a total of 2 minutes to form colostrum; move to high-pressure homogenization Homogenize the high-pressure emulsion in the machine, and circulate it 5 times at 3000psi to obtain the nanoemulsion; use a rotary evaporator to volatilize the organic solvent below 37°C, and the obtained suspension is translucent, and transfer it to a 5ml vial, 1ml / In addition, 1ml of 20% ma...

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Abstract

The invention provides an albumin-combined taxol long-circulation nano-particle freeze-dried preparation. Compared with a conventional taxol injecting solution and conventional albumin-combined taxol long-circulation nano-particles, the albumin-combined taxol long-circulation nano-particle freeze-dried preparation can improve a targeting performance of taxol on tumor, is enhanced in effects and is reduced in toxic and side effects. The invention also provides a preparation method of the albumin-combined taxol long-circulation nano-particle freeze-dried preparation.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an albumin-bound paclitaxel nanoparticle freeze-dried preparation with tumor targeting and long-circulation effect. Background technique [0002] Paclitaxel is a secondary metabolite with anti-tumor activity extracted from the Taxus genus. It is a white, odorless crystal or powder, insoluble in water, and easily soluble in organic solvents such as acetone, chloroform, and ether. Paclitaxel is a complex diterpenoid compound with an oxygen-containing tetracyclic taxane ring and an ester side chain. The chemical name is: 5β, 20-epoxy-1, 2α, 4, 7β, 1β, 13α-hexahydroxyl Taxane-11-en-9-one-4,10-diacetate-2-benzoate-13[(2R,3S)]-N-benzoyl-3-phenylisoserine ester , the molecular formula is C 47 h 51 NO 14 , Molecular weight: 853.906. It was discovered at the American Cancer Institute in 1963. Monroe E.Wall and Mansukh C.Wani isolated this substance from the bark of Pacific yew (Taxus brevifol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/337A61K47/42A61P35/00
Inventor 金义光杜丽娜李淼冯雪金仁熙
Owner ACADEMY OF MILITARY MEDICAL SCI
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