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A long-circulating liposome freeze-dried preparation of deoxypodophyllotoxin

A long-circulating liposome, deoxypodophyllotoxin technology, applied in the directions of liposome delivery, freeze-dried delivery, antiviral agents, etc., can solve the problem of increasing drug time, low targeting, and stability of common liposomes Sexual problems, etc.

Active Publication Date: 2017-11-14
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the unsatisfactory stability of ordinary liposomes and low targeting, we made deoxypodophyllotoxin into long-circulating liposomes and delivered them to the body, which can increase the drug’s circulation time in the body and better passively target the drug to Tumor site, improve the anti-tumor effect of the drug and reduce its toxicity

Method used

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  • A long-circulating liposome freeze-dried preparation of deoxypodophyllotoxin
  • A long-circulating liposome freeze-dried preparation of deoxypodophyllotoxin
  • A long-circulating liposome freeze-dried preparation of deoxypodophyllotoxin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Party:

[0024] Deoxypodophyllotoxin 9mg, soybean lecithin 50mg, cholesterol 10mg, polyethylene glycol-distearoylphosphatidylethanolamine 5mg

[0025] Preparation:

[0026] Put deoxypodophyllotoxin, soybean lecithin, cholesterol, polyethylene glycol-distearoylphosphatidylethanolamine in an eggplant-shaped bottle, add 20ml of chloroform to dissolve completely, heat in a water bath at 40°C and evaporate under reduced pressure to trichloro The methane was exhausted, and it was attached to the bottom of the bottle in the form of a transparent film. Add 30ml of water, heat in a water bath at 20°C, and spin the film to hydrate for 20 minutes to obtain an opalescent liposome solution.

Embodiment 2

[0028] Party:

[0029] Deoxypodophyllotoxin 9mg, soybean lecithin 200mg, cholesterol 20mg, polyethylene glycol-distearoylphosphatidylethanolamine 20mg

[0030] Preparation:

[0031] Put deoxypodophyllotoxin, soybean lecithin, cholesterol, polyethylene glycol-distearoylphosphatidylethanolamine in an eggplant-shaped bottle, add 20ml of chloroform to dissolve completely, heat in a water bath at 40°C and evaporate under reduced pressure to trichloro The methane was exhausted, and it was attached to the bottom of the bottle in the form of a transparent film. Add 30ml of water, heat in a water bath at 40°C, and spin the film to hydrate for 20 minutes to obtain an opalescent liposome solution.

Embodiment 3

[0032] Example 3 Preparation of deoxypodophyllotoxin long-circulating liposomes without lyoprotectant

[0033] Party:

[0034] Deoxypodophyllotoxin 9mg, soybean lecithin 108mg, cholesterol 12mg, polyethylene glycol-distearoylphosphatidylethanolamine 6.5mg

[0035] Preparation:

[0036] Put deoxypodophyllotoxin, soybean lecithin, cholesterol, polyethylene glycol-distearoylphosphatidylethanolamine in an eggplant-shaped bottle, add 20ml of chloroform to dissolve completely, heat in a water bath at 40°C and evaporate under reduced pressure to trichloro Methane is exhausted, and it is attached to the bottom of the bottle in the form of a transparent film. Add 30ml of water, heat in a water bath at 40°C, rotate the film to hydrate for 20min, and obtain an opalescent liposome solution. Filter it with a 0.22μm filter membrane, and the filtrate is 10ml per bottle. Packed in vials, freeze-dried to obtain white loose powder.

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Abstract

The invention provides a deoxidated podophyllotoxin long-circulating liposome freeze-drying preparation. The method for preparing the deoxidated podophyllotoxin long-circulating liposome comprises the following steps: dissolving deoxidated podophyllotoxin, phospholipid, cholesterol and polyethylene glycol-distearoyl Phosphoethanolamine in an organic solvent, displacing the solvent into the film, hydrating to obtain lipidosome, and further preparing the freeze-drying preparation. The freeze-drying preparation can be used for treating tumors, the drug-loading encapsulation efficiency is over 90 percent, the particle size of the redissolved lipidosome is 95-125nm, and the redissolved lipidosome solution can be stabilized at the temperature of 25 DEG C for 8-24 hours.

Description

technical field [0001] The invention relates to a freeze-dried drug long-circulation liposome and a preparation method thereof, in particular to a preparation method of a deoxypodophyllotoxin-loaded long-circulation liposome and a freeze-dried preparation thereof. Background technique [0002] Deoxypodophyllotoxin is a compound extracted and purified from lignin plants, and its structural formula is as follows: [0003] [0004] Experimental reports in the 1990s have confirmed that deoxypodophyllotoxin has an in vitro inhibitory effect on cell lines of P-388 leukemia, human lung cancer A-549, human nasopharyngeal carcinoma KB and colon cancer HT-29, and has a certain Hepatoprotective and antiviral effects. Since deoxypodophyllotoxin is insoluble in water and slightly soluble in ethanol and ether, it cannot be directly used to prepare intravenous injection preparations, and it is difficult to prepare liposomes by injection, which limits its application in the preparation ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/19A61K31/365A61P35/00A61P35/02A61P1/16A61P31/12
Inventor 周建平王舒丁杨
Owner CHINA PHARM UNIV