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Venenum bufonis nanometer long-circulating liposome and preparation method thereof

A technology of long-circulating liposomes and toadstools, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations of inactive ingredients, etc., can solve the problems of reduced application value, drug leakage, easy rupture, etc. Beneficial for disease treatment, prolonging time and avoiding phagocytosis

Inactive Publication Date: 2012-05-23
SHANGHAI INST OF PHARMA IND CO LTD
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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
Comparison scheme
Effect test

Embodiment 1

[0043] Dissolve 40 mg of toad venom extract, 1000 mg of soybean lecithin, 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] 500 mg of poloxamer 188 was dissolved in 50 ml of phosphate buffered saline (PBS) at pH=7.4 to obtain solution B.

[0045] Add solution A drop by drop into solution B which is protected by nitrogen gas and stirred rapidly, stir at 40°C for 60 minutes, then remove ethanol by rotary evaporation, homogenize under high pressure, filter, and freeze-dry by conventional methods to obtain the long-circulated toad venom nanometer of the present invention. Liposomes.

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

Embodiment 2

[0048] Dissolve 40mg of toad venom extract, 1000mg of soybean lecithin, 10mg of cholesterol and 50mg of polyethylene glycol 4000 in 5ml of ethanol to obtain solution A. Others are the same as in Example 1, that is, the nano-long circulation liposome of Bufoni venom of the present invention is obtained. The obtained toad venom nano long circulation liposome has an average particle diameter of 20nm.

Embodiment 3

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

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PUM

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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 nanometer long circulation liposome of toadstool and a preparation method thereof. Background technique [0002] Toad venom is the white slurry secreted by the posterior ear glands and skin glands of Bufo bufo or Bufo bufo, which is processed and dried. Ancient and modern prescriptions widely use toads and toads to remove toxins and reduce swelling, relieve pain and kill insects, strengthen the heart and diuresis. Through modern scientific research, it has been found that the mixture of three fat-soluble components of toad bufogenin, cinobufagin and bufalin not only has obvious anti-tumor effect, but also can transform tumor cells into normal cells (induced Tumor cell differentiation), inducing tumor cell apoptosis, inhibiting tumor cell angiogenesis, reducing tumor metastasis, etc., especially has a good effect on lymphocytic leukemia (Edited by Jiang Kaixian, Clinical and Research o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K35/56A61K47/24A61P35/00A61K35/65
Inventor 奉建芳祝林李瑞新
Owner SHANGHAI INST OF PHARMA IND CO LTD
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