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Irinotecan nano circulating liposome and preparation method thereof

A nano-liposome and irinotecan technology, applied in the field of biomedicine, can solve the problems of low encapsulation rate, instability, uneven particle size distribution of liposomes, etc., and achieves easy industrialization, is conducive to absorption, and solves The effect of uneven particle size distribution

Inactive Publication Date: 2011-12-28
中华人民共和国卫生部肝胆肠外科研究中心 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0021] In view of the defects of uneven particle size distribution, low encapsulation efficiency and instability of liposomes prepared in the prior art, the present invention provides a combination of ethanol injection method and ammonium sulfate gradient active drug loading method to prepare irinotecan long-circulation nano-lipid A New Approach to Plastid Drugs

Method used

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  • Irinotecan nano circulating liposome and preparation method thereof
  • Irinotecan nano circulating liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Preparation of irinotecan long-circulation nanoliposomes.

[0040] Select PEG-DSPE as an additional agent for preparing long-circulating liposomes, and phospholipids, cholesterol, poloxamer 188, V E Dissolved in an ethanol solution, injected into the ammonium sulfate solution in which PEG-DSPE was dissolved under the condition of stirring in a water bath at 55°C, the concentration of phospholipids was 100 mg / ml, and the mass ratio of phospholipids, cholesterol, poloxamer 188, and PEG-DSPE was 3: 1:0.6:0.3, pass N 2 Under the condition of incubating and stirring for 0.5-1h, the obtained long-circulation blank liposomes were dialyzed overnight in normal saline, the pH of the external phase was adjusted to be 7-7.5, and the irinotecan solution was added under the condition of 55°C water bath (irinotecan / phospholipid mass ratio 1 :10) Incubate for 5-15min to obtain irinotecan long-circulation nanoliposomes.

[0041] The irinotecan long-circulation nanoliposomes...

Embodiment 2

[0045] Embodiment 2, the preparation of irinotecan long circulation nano liposome

[0046] Select PEG2000 as an additional agent for preparing long-circulating liposomes, and phospholipids, cholesterol, poloxamer 188, V E Dissolved in ethanol solution, injected into the ammonium sulfate solution in which PEG2000 was dissolved under the condition of stirring in a water bath at 55°C, the concentration of phospholipids was 100 mg / ml, and the mass ratio of phospholipids, cholesterol, poloxamer 188, and PEG2000 was 10:5:2: 1, pass N 2 Under the condition of incubating and stirring for 0.5-1h, the obtained long-circulation blank liposomes were dialyzed overnight in normal saline, the pH of the external phase was adjusted to 7.5, and irinotecan solution was added under the condition of 55°C water bath (irinotecan / phospholipid mass ratio 1:10 ) was incubated for 5-15 minutes to obtain irinotecan long-circulation nanoliposomes.

[0047] The particle size of irinotecan long-circulatio...

Embodiment 3

[0048] Embodiment 3, the preparation of irinotecan long circulation nano liposome injection

[0049] The obtained irinotecan long-circulation nanoliposomes prepared in Examples 1 and 2 are filtered and sterilized by a microporous membrane, filled with nitrogen and filled in an ampoule vial to obtain the injection of irinotecan long-circulation nanoliposomes liquid.

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Abstract

The invention provides a novel Irinotecan carrier which is circulating nano liposome and a novel preparation method thereof which is an ethanol injection-ammonium sulfate active medicament-loading method. The preparation process comprises: a, dissolving a lipid material for forming the liposome in ethanol to prepare solution; b, dissolving a polyethylene glycol compound in solution of ammonium sulfate to prepare a hydration medium; c, injecting solution obtained by the step a into the hydration medium obtained by the step b with stirring in a water bath, stirring at a constant temperature fora certain period under a condition of introducing N2 to form circulating blank liposome; d, dialyzing the blank liposome obtained by the step c in physiological saline; and e, adding solution of Irinotecan into the blank liposome, regulating the pH value of an external phase, and performing incubation and medicament loading at a certain temperature to obtain the Irinotecan circulating nano liposome. The process is simple, the particle size is 80 to 150 nanometers, the coating rate is over 95 percent, the sterile preparation can be obtained easily, and an industrialization requirement is met.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a new method for preparing irinotecan long-circulation nano liposomes. Background technique [0002] Irinotecan (hydroxycamptothecin-11, CPT-11) is a levorotatory trace alkaloid extracted and isolated from the natural and unique plant Camptotheca involucrata in my country. It is a semi-synthetic soluble camptothecin derivative. Constructase I (Topo-1) Inhibitors [1] , Irinotecan and its metabolite SN-38 cause DNA single-strand breaks through the stable combination with the DNA-Topo-1 complex, resulting in irreversible damage to the DNA and death. Studies have shown that the content of Topo-1 in a variety of tumor cells, especially colorectal cancer, cervical cancer, ovarian cancer, etc., is much higher than that in normal tissues. Selectivity, so as to exert its specific anti-tumor activity and reduce its toxicity to normal cells. As a new type of anti-tumor drug, since it ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/4745A61K47/34A61K47/24A61K47/28A61P35/00A61K47/10
Inventor 张阳德何剪太李坚陈长生刘勇陈玉祥何颖
Owner 中华人民共和国卫生部肝胆肠外科研究中心
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