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Podophyllotoxin ethosomes and preparation methods thereof

A technology of podophyllotoxin and alcohol plastids, which is applied in the directions of liposome delivery, antiviral agents, pharmaceutical formulations, etc., can solve problems such as difficulty in eliminating recurrence, toxic and side effects, etc.

Inactive Publication Date: 2011-08-10
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although podophyllotoxin tincture can remove visible lesions, excessive use on a large area will cause serious toxic side effects, and although liposomes can reduce adverse reactions, their effects are limited to the surface layer of the skin, so it is difficult to eliminate lesions deep in the skin. HPV latent infection leading to its recurrence

Method used

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  • Podophyllotoxin ethosomes and preparation methods thereof
  • Podophyllotoxin ethosomes and preparation methods thereof
  • Podophyllotoxin ethosomes and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Weigh 35mg of podophyllotoxin, 0.5g of soybean lecithin (phosphatidylcholine content > 95%) and place in an airtight container, add 3mL of absolute ethanol and place on a magnetic stirrer, and stir at 37°C and 700rpm under airtight conditions While slowly injecting 2 times the amount of water, continue to stir for 5 minutes after injection, then ultrasonically probe for 0.5 hours in an ice-water bath, and finally pass through a 0.45 μm microporous membrane to obtain the product.

[0029] After testing, the average particle size of the podophyllotoxin ethosomes prepared in this example was 83 nm, and the encapsulation efficiency was 51%.

Embodiment 2

[0031] Weigh 35 mg of podophyllotoxin, 0.5 g of soybean lecithin (phosphatidylcholine content > 95%) and dissolve in 5 mL of methanol: chloroform (volume ratio of 3: 1) mixed solvent, and place the solution in 500 mL of ground eggplant type In the bottle, use a rotary evaporator to remove the solvent under reduced pressure at a water bath temperature of 37°C, and keep it in vacuum for 30 minutes to make the lipids form a uniform film on the wall of the vessel. Sonicate the probe in an ice-water bath for 5 minutes, and pass through a 0.22 μm microporous membrane to obtain the product.

[0032] After testing, the average particle size of the podophyllotoxin ethosomes prepared in this example was 80 nm, and the encapsulation efficiency was 49.5%.

Embodiment 3

[0034] Weigh 30 mg of podophyllotoxin, 0.5 g of soybean lecithin (phosphatidylcholine content > 95%) and dissolve in 3 mL of methanol: chloroform (volume ratio 4: 1) mixed solvent, and place the solution in 500 mL of ground eggplant type In the bottle, use a rotary evaporator to remove the solvent under reduced pressure at a water bath temperature of 37°C, and keep it in vacuum for 30 minutes, so that the lipids form a uniform film on the wall of the vessel, add 8 mL of 35% ethanol aqueous solution, rotate and hydrate for 30 minutes, and place at room temperature. Sonicate the probe in an ice-water bath for 2 minutes, pass through a 0.50 μm microporous membrane, and obtain it.

[0035] After testing, the average particle size of the podophyllotoxin ethosomes prepared in this example was 157 nm, and the encapsulation efficiency was 80.3%.

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Abstract

The invention discloses podophyllotoxin ethosomes. Podophyllotoxin is encapsulated in ethosomes, and a medicine carrying lipid material is phosphatidylcholine, phosphatidylethanolamine or dipalmitoylphosphatidylcholine, wherein the grain diameter of the lipid material is between 50 and 300 nanometers. The podophyllotoxin ethosomes can be prepared into external preparations such as patches, gel and the like, and can reduce medicinal dose, and fulfill the aims of increasing curative effect and reducing relapse and toxic and side effects. The invention also discloses two preparation methods for the podophyllotoxin ethosomes.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a podophyllotoxin ethosome; the invention also relates to a preparation method of the etosome. Background technique [0002] Podophyllotoxin (PPT) is a lignan compound extracted and isolated from the roots and rhizomes of the Berberidaceae plants Peach ear seven, star anise lotus or hexagon lotus, it is recommended by the World Health Organization (WHO) to treat genital warts (CA) first-line drug, its main mechanism of action is to kill cells infected by human papilloma (HPV) through its cytotoxicity, commonly used is 0.5% podophyllotoxin tincture. [0003] CA accounts for the second place of sexually transmitted diseases in my country. The cause of CA is that after HPV infects the human body, it resides in the nucleus of stratum corneum forming cells such as basal cells, and its DNA can be integrated into the DNA of the host cell and expressed, resulting in excessive epidermal hyperplasia ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/365A61K47/24A61P31/20A61P17/12
Inventor 冯年平于燕燕赵继会翁海挺施晓琴
Owner SHANGHAI UNIV OF T C M
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