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Nanometer drug delivery system carrying tanshinone IIA

A drug delivery system and technology containing Danshen, which is applied in the direction of pharmaceutical formulations, antineoplastic drugs, drug combinations, etc., can solve the problems of limiting the use of tanshinone IIA, insoluble in water, short half-life, etc., to achieve good therapeutic effect and good targeting effect, the effect of reducing toxicity

Inactive Publication Date: 2013-05-22
SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, tanshinone Ⅱ A is a fat-soluble non-quinone component, which is insoluble in water. After administration in vivo, it reaches the peak plasma concentration in a short time and has a short half-life. After administration, the drug is widely distributed in the stomach, small intestine, liver, lungs, pancreas, etc. in multiple organs and is rapidly cleared out of the body
This pharmacokinetic characteristic limits the use of tanshinone Ⅱ A in the field of tumor therapy

Method used

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  • Nanometer drug delivery system carrying tanshinone IIA
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  • Nanometer drug delivery system carrying tanshinone IIA

Examples

Experimental program
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Effect test

Embodiment 1

[0047] Example 1: The molar ratio of lactic acid and glycolic acid is 50:50, the molar ratio of glycolic acid and lysine is 70:10, the molar ratio of mPEG-PLGA-PLL and cRGD is 1:20, TSIIA and mPEG-PLGA-PLL- The molar ratio of cRGD is 1:20.

Embodiment 2

[0048] Example 2: The molar ratio of lactic acid and glycolic acid is 70:30, the molar ratio of glycolic acid and lysine is 6:10, the molar ratio of mPEG-PLGA-PLL and cRGD is 1:30, TSIIA and mPEG-PLGA-PLL- The molar ratio of cRGD is 1:30.

Embodiment 3

[0049] Example 3: The molar ratio of lactic acid and glycolic acid is 80:20, the molar ratio of glycolic acid and lysine is 50:20, the molar ratio of mPEG-PLGA-PLL and cRGD is 1:50, TSIIA and mPEG-PLGA-PLL- The molar ratio of cRGD is 1:5.

[0050] Take any one of the proportions in Example 1 to Example 3, and prepare polyethylene glycol modified with valine-arginine-glycine-aspartic acid-glutamic acid cyclic peptide (cRGD) according to the following method Tanshinone IIA (TSIIA)-loaded nanoparticles supported by monomethyl ether-polylactic-glycolic acid-polylysine (mPEG-PLGA-PLL) polymer.

[0051] Step 1, such as figure 1 cRGD-modified mPEG-PLGA-PLL-cRGD was prepared as indicated. Among them, h is hour, d is day, LA is lactide, Sn(Oct) 2 is stannous octoate, mPEG is polyethylene glycol monomethyl ether, PLGA is polylactic acid / glycolic acid, DCC is dicyclohexylcarbodiimide, DMAP is 4-dimethylaminopyridine, BOC is phenylalanine, HAc is acetic acid, HBr is hydrobromic acid, ...

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Abstract

The invention discloses a nanometer drug delivery system carrying tanshinone IIA, wherein the nanometer drug delivery system is a nanoparticle carrying the tanshinone IIA, which takes methoxy polyethylene glycol-polylactic acid glycolic acid-polylysine polymer modified by valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide as a carrier; the diameter of the nanoparticle is 10-2000nm; and the molecular weight of the polymer is 1.5*103-9.5*106. The molar ratio of the tanshinone IIA and the carrier polymer is 1-60:1-60; the molar ratio of lactic acid in the polymer and the glycolic acid is 1-80:1-80; the molar ratio of the glycolic acid and the lysine is 90-50:10-50; and the molar ratio of the methoxy polyethylene glycol-polylactic acid glycolic acid-polylysine and the valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide is 1-60:1-60. The nanometer drug delivery system carrying the tanshinone IIA can effectively lower the toxicity of the tanshione IIA and increases the targeting of the tanshinone IIA and the treatment effect.

Description

technical field [0001] The invention relates to a nano drug delivery system, in particular to a nano drug delivery system loaded with tanshinone IIA. Background technique [0002] Nanoparticles prepared by nanotechnology have a large specific surface area, the number of surface atoms, surface energy and surface tension increase sharply with the decrease of particle size, and there are strong or weak interactions between nano units. These characteristics make nano Particles have small size effect, surface effect, strong adsorption and biological activity, exhibit many excellent properties and new functions, can be used as drug carriers, change the distribution characteristics of drugs in vivo, and improve drug absorption, availability and stability. Improving the properties and targeting of drugs, sustained drug release, prolonged drug action time, reduced drug doses, reduced or avoided side effects, and good for storage. It is used in the treatment of diseases and is a new d...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/58A61K47/34A61P35/00C08G65/48C08G63/91
Inventor 王炎李琦范忠泽孙珏殷佩浩陈红宇宋大迁靳永杰颜琳琳
Owner SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE PUTUO DISTRICT CENT HOSPITAL
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