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Liposome composition for resisting tumors

A liposome composition and anti-tumor technology, applied in the field of anti-tumor liposome compositions, can solve the problems of high bioavailability, low drug loading, inability to solve targeting, etc., and achieve the effect of inhibiting tumors

Active Publication Date: 2014-07-23
卢凯华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Liposomes have the advantages of long-acting, reducing toxicity and protecting encapsulated drugs, but there are also some disadvantages: the targeting of general liposomes is mainly concentrated in organs rich in reticuloendothelial cells, if you want to treat other tissues and organs Treatment of its targeting is not obvious; the stability of liposomes is not enough, the liposomes prepared by conventional methods are easy to aggregate and fuse, and the validity period is short; the leakage of liposome contents, usually liposomes in the preservation process , the content will leak more or less, especially for some water-soluble drugs; for different drugs, the encapsulation efficiency and drug loading of liposomes vary greatly, and the drug loading of some drugs is extremely low. It is difficult to play the role of drugs
[0004] The preventive health care effect of resveratrol on cardiovascular diseases and tumors has caused in-depth research, but because resveratrol is insoluble in water and unstable to light and other defects, its absorption in the body is poor and its bioavailability is high, so As a result, the clinical effect is not ideal. At present, there are studies on resveratrol liposomes in the literature, but the use methods are relatively traditional, and problems such as targeting, liposome stability, and leakage cannot be solved.

Method used

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  • Liposome composition for resisting tumors

Examples

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Effect test

Embodiment 1

[0022] A preparation method for an anti-tumor liposome composition, specifically comprising the following steps:

[0023] 1) Weigh 21g of allicin, 7g of resveratrol, 10g of hydrogenated saturated soybean lecithin, 0.25g of cholesterol, 0.75g of cyclodextrin, 0.025g of RGD peptide-6-aminocaproic acid arm complex, and 0.5g of DSPC-PEG2000 , non-ionic surfactant 100g;

[0024] 2) Synthesis of targeting RGD peptide-6-aminocaproic acid arm complex: RGD peptide-6-aminocaproic acid arm complex was synthesized by solid-phase synthesis, and the RGD peptide sequence was: glycine-alanine-arginine- Tyrosine-cysteine-arginine-glycine-aspartic acid-cysteine-phenylalanine-aspartic acid-glycine;

[0025] 3) Combine the weighed resveratrol and allicin with hydrogenated saturated soybean lecithin, cholesterol, cyclodextrin, RGD peptide-6-aminocaproic acid arm complex, DSPC-PEG2000 and non-ionic surface Dissolve the active agent in ether, add 150ml of PBS, and stir ultrasonically in an ice-wat...

Embodiment 2

[0027] A preparation method for an anti-tumor liposome composition, specifically comprising the following steps:

[0028] 1) Weigh 29g of allicin, 7g of resveratrol, 10g of hydrogenated saturated lecithin, 0.3g of cholesterol, 1.2g of glucose, 0.030g of RGD peptide-6-aminocaproic acid arm complex, 0.6g of DSPC-PEG2000, non Ionic surfactant 100g;

[0029] 2) Synthesis of targeting RGD peptide-6-aminocaproic acid arm complex: RGD peptide-6-aminocaproic acid arm complex was synthesized by solid-phase synthesis, and the RGD peptide sequence was: glycine-alanine-arginine- Tyrosine-cysteine-arginine-glycine-aspartic acid-cysteine-phenylalanine-aspartic acid-glycine;

[0030] 3) Combine the weighed resveratrol and allicin with hydrogenated saturated lecithin, cholesterol, glucose, RGD peptide-6-aminocaproic acid arm complex, DSPC-PEG2000 and non-ionic surfactant Dissolve in ether, add 150ml of PBS, and stir ultrasonically in an ice-water bath to form an emulsion. At room temperatur...

Embodiment 3

[0032] A preparation method for an anti-tumor liposome composition, specifically comprising the following steps:

[0033] 1) Weigh 24g of allicin, 6g of resveratrol, 10g of distearoylphosphatidylcholine, 0.4g of cholesterol, 0.8g of sorbitol, 0.028g of RGD peptide-6-aminocaproic acid arm complex, DSPC-PEG2000 0.55g, non-ionic surfactant 100g;

[0034] 2) Synthesis of targeting RGD peptide-6-aminocaproic acid arm complex: RGD peptide-6-aminocaproic acid arm complex was synthesized by solid-phase synthesis, and the RGD peptide sequence was: glycine-alanine-arginine- Tyrosine-cysteine-arginine-glycine-aspartic acid-cysteine-phenylalanine-aspartic acid-glycine;

[0035] 3) Mix resveratrol and allicin, which have been weighed, with distearoylphosphatidylcholine, cholesterol, sorbitol, RGD peptide-6-aminocaproic acid arm complex, DSPC-PEG2000 and Dissolve the non-ionic surfactant in ether, add 150ml of PBS, and stir ultrasonically in an ice-water bath to form an emulsion. At room ...

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Abstract

The invention provides a liposome composition for resisting tumors. The liposome composition is characterized in that allicin and resveratrol are filled in the liposome composition. The invention also provides a method for preparing the liposome composition. According to the liposome composition, the problems of low and unstable encapsulation rate when multiple components are encapsulated can be solved by process regulation, and an extremely good effect for inhibiting tumors can be achieved by virtue of drug effect researches, and a new chapter of the anti-tumor liposome field is opened.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to a liposome composition for antitumor. Background technique [0002] Liposomes are bilayer vesicles that resemble biological membranes. Since the first report of the liposome structure by British scholar Bangham et al. in the 1960s, liposomes have received more and more attention. In 1971, British scientists Rymen and others began to use liposomes as drug carriers, which made them widely used in the field of pharmacy and rapidly developed into a new type of drug delivery system. Liposomes have the advantages of long-acting, reducing toxicity and protecting encapsulated drugs, but there are also some disadvantages: the targeting of general liposomes is mainly concentrated in organs rich in reticuloendothelial cells, if you want to treat other tissues and organs Treatment of its targeting is not obvious; the stability of liposomes is not enough, the liposomes prepared by c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/255A61K9/48A61K9/127A61K47/42A61P35/00A61K31/05
Inventor 卢凯华何靓张梅玲
Owner 卢凯华
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