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Venenum bufonis nanometer long-circulating liposome and preparation method thereof

A technology for long-circulating liposomes and toadstools, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations with inactive ingredients, etc., can solve problems such as easy rupture, reduced application value, drug leakage, etc. Phagocytosis, beneficial to disease treatment, prolonged effect

Inactive Publication Date: 2010-06-16
SHANGHAI INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after liposomes enter the circulatory system, due to the action of proteins, opsonins, antibodies, enzymes, etc. in the blood, they are prone to rupture, and the encapsulated drugs leak quickly and are recognized and absorbed by the reticuloendothelial system (RES). thereby reducing the application value

Method used

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  • Venenum bufonis nanometer long-circulating liposome and preparation method thereof
  • Venenum bufonis nanometer long-circulating liposome and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0043] Dissolve 40 mg of toad venom extract, 1000 mg of soybean phospholipids, 10 mg of cholesterol, and 10 mg of polyethylene glycol-distearoylphosphatidylcholine (PEG-DSPC) (molecular weight 6000) in 5 ml of ethanol to obtain solution A.

[0044] Dissolve 500 mg of Poloxamer 188 in 50 ml of phosphate buffered saline (PBS) with pH=7.4 to obtain solution B.

[0045] The A solution was dropped into the B solution protected by nitrogen and rapidly stirred, stirred at 40°C for 60 minutes, then the ethanol was removed by rotary evaporation, homogenized under high pressure, filtered, and freeze-dried by conventional methods to obtain the toad venom nano-long loop of the present invention. Liposomes.

[0046] The particle size of the obtained toad venom nano-long circulating liposome was determined by the above method, and the average particle size was 50 nm, and no particles larger than 200 nm were found. Its particle size distribution is as figure 1

Embodiment 2

[0048] 40 mg of toad venom extract, 1000 mg of soybean lecithin, 10 mg of cholesterol and 50 mg of polyethylene glycol 4000 were dissolved in 5 ml of ethanol to obtain solution A. Others are the same as in Example 1, that is, toad venom nano-long circulating liposomes of the present invention are prepared. The average particle size of the obtained toad venom nano-long circulating liposomes was 20 nm.

Embodiment 3

[0050] Dissolve 40 mg of toad venom extract, 1000 mg of soybean phospholipids, 10 mg of cholesterol and 10 mg of polyethylene glycol-phosphatidylethanolamine (PEG-PE) (molecular weight 10000) in 5 ml of ethanol to obtain solution A. Others are the same as in Example 1, that is, toad venom nano-long circulating liposomes of the present invention are prepared. The average particle size of the obtained toad venom nano-long circulating liposome is 100 nm.

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Abstract

The invention discloses a venenum bufonis nanometer long-circulating liposome and a preparation method thereof. The venenum bufonis nanometer long-circulating liposome comprises the following components in part by weight: 1 part of venenum bufonis extract, 10-100 parts of phosphatide, 1-10 parts of cholesterol, 0.1-50 parts of surfactant and 0.1-10 parts of film-modified material. The venenum bufonis nanometer long-circulating liposome effectively prolongs the stay time of an active component of venenum bufonis in the blood of the body, reduces the highest concentration of a medicament, has remarkably lower toxicity than that of the traditional product, has the target treatment effect and uniform distribution of granularity of products, and can be used for treating various tumor diseases.

Description

Technical field [0001] The invention relates to a liposome preparation, in particular to a toad venom nano-long circulating liposome and a preparation method thereof. Background technique [0002] Toad vulgaris is a white slurry secreted by the posterior ear glands and skin glands of Bufo bufo or black-orbited toad, which is processed and dried. The ancient and modern proven prescriptions are widely used in toad and toad venom to remove toxin and reduce swelling, relieve pain and kill insects, strengthen heart and diuresis. Through modern scientific research, it has been discovered that the mixture of the three fat-soluble components of Bubufaxin, Bufaxin and Bufafalin in Bufo venom not only has obvious anti-tumor effect, but also can transform tumor cells into normal cells (inducing Tumor cell differentiation), inducing tumor cell apoptosis, inhibiting tumor cell angiogenesis, reducing tumor metastasis, etc., especially for lymphocytic leukemia (edited by Jiang Kaixian, clinica...

Claims

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Application Information

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IPC IPC(8): A61K35/56A61K9/127A61K47/24A61P35/00A61K35/65
Inventor 奉建芳祝林李瑞新
Owner SHANGHAI INST OF PHARMA IND
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