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Preparation method of nanometer drug delivery system carrying tanshinone IIA and application thereof

A drug delivery system and a technology containing salvia miltiorrhiza, applied in medical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as short half-life, limited use of tanshinone ⅡA, insoluble in water, etc. , to achieve the effect of reducing toxicity, enhancing targeting and therapeutic effect

Inactive Publication Date: 2013-05-22
SHUGUANG HOSPITAL AFFILIATED WITH SHANGHAI UNIV OF T C M
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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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  • Preparation method of nanometer drug delivery system carrying tanshinone IIA and application thereof
  • Preparation method of nanometer drug delivery system carrying tanshinone IIA and application thereof
  • Preparation method of nanometer drug delivery system carrying tanshinone IIA and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] 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

[0050] 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

[0051] 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.

[0052] 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.

[0053] 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 preparation method of a nanometer drug delivery system carrying tanshinone IIA. The preparation method comprises the following steps: step 1. preparing methoxy polyethylene glycol-polylactic acid glycolic acid-polylysine modified by valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide; and step 2. preparing methoxy polyethylene glycol-polylactic acid glycolic acid-polylysine nanoparticle carrying the tanshione IIA and modified by the valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide when the molar ratio of the methoxy polyethylene glycol-polylactic acid glycolic acid-polylysine nanoparticle modified by the valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide and the tanshinone IIA is 1-60:1-60. The invention also discloses the application for the nanometer drug delivery system carrying the tanshinone IIA prepared by the method. The nanometer drug delivery system carrying the tanshinone IIA prepared by the method can effectively lower the toxicity of the tanshinone IIA and increase the targeting of the tanshinone IIA and the treatment effect.

Description

technical field [0001] The present invention relates to a preparation method and application of a nanometer drug delivery system, in particular to a nanometer drug delivery system loaded with tanshinone IIA, a preparation method and application of a nanometer 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/58A61K47/34A61P35/00
Inventor 王炎李琦朱惠蓉秦建民范忠泽周利红陈红宇宋大迁叶乃菁
Owner SHUGUANG HOSPITAL AFFILIATED WITH SHANGHAI UNIV OF T C M
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