Tanshinone IIAPEG-PLGA-PEG (Tanshinone Polyethylene Glycol-Poly(Lactic-Co-Glycolic Acid)-Polyethylene Glycol) nanoparticles and preparation method thereof

A technology of tanshinone and nanoparticles, which is applied in the field of medicine, can solve the problems of reaching the target site and difficult drugs, and achieve the effects of changing distribution, avoiding side effects, and prolonging the half-life of blood

Inactive Publication Date: 2017-09-05
HARBIN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the PLGA block has strong crystallinity and hydrophobicity, it is very easy to be cleared by RES, and it is difficult for the drug to reach the target site

Method used

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  • Tanshinone IIAPEG-PLGA-PEG (Tanshinone Polyethylene Glycol-Poly(Lactic-Co-Glycolic Acid)-Polyethylene Glycol) nanoparticles and preparation method thereof
  • Tanshinone IIAPEG-PLGA-PEG (Tanshinone Polyethylene Glycol-Poly(Lactic-Co-Glycolic Acid)-Polyethylene Glycol) nanoparticles and preparation method thereof
  • Tanshinone IIAPEG-PLGA-PEG (Tanshinone Polyethylene Glycol-Poly(Lactic-Co-Glycolic Acid)-Polyethylene Glycol) nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Preparation of Tanshinone IIA PEG-PLGA-PEG Nanoparticles Encapsulated

[0030] (1) 2 mg of tanshinone IIA and 30 mg of PEG-PLGA-PEG were ultrasonically dissolved in a mixed solvent of 2 ml of acetone and dichloromethane (acetone:dichloromethane = 1:9) as the oil phase, and the prepared mass fraction was 0.5% The poloxamer F188 solution is used as the aqueous phase;

[0031] (2) Under the condition of stirring in an ice-water bath, use a syringe to draw 30 μL of the inner aqueous phase in step (1) and drop it into the organic phase at a speed of 10-30 drops / min, sonicate for 5 s, intermittently for 5 s, and continuously sonicate for 10 min the formation of colostrum;

[0032] (3) Under the condition of stirring in an ice-water bath, draw the colostrum in step (2) with a syringe, and add dropwise to 20 ml 0.5% polo at a rate of 10-30 drops / min. In Sharm F188 solution (the ratio of colostrum to double milk is 1:10), ultrasonication was performed for 5 s, interm...

Embodiment 2

[0034] Example 2 Preparation of Tanshinone IIA PEG-PLGA-PEG Nanoparticles Encapsulated

[0035] (1) Sonicate 4 mg of tanshinone IIA and 30 mg of PEG-PLGA-PEG in a mixed solvent of 2 ml of acetone and methylene chloride (acetone: methylene chloride = 1:8) as the oil phase, and prepare a mass fraction of 0.5% The Tween-80 solution is used as the water phase;

[0036] (2) Under the condition of stirring in an ice-water bath, use a syringe to draw 30 μL of the inner aqueous phase in step (1) and drop it into the organic phase at a speed of 10-30 drops / min, sonicate for 5 s, intermittently for 5 s, and continuously sonicate for 10 min the formation of colostrum;

[0037] (3) Under the condition of stirring in an ice-water bath, draw the colostrum in step (2) with a syringe, and add it dropwise to 20 ml 0.5% Tween at a rate of 10-30 drops / min. -80 solution, ultrasonic 5 s intermittent 5 s, continuous ultrasonic 20 min to form double emulsion;

[0038] (4) Stir at room temperature...

Embodiment 3

[0039] Example 3 Preparation of Tanshinone IIA PEG-PLGA-PEG Nanoparticles Encapsulated

[0040] (1) Sonicate 8 mg of tanshinone IIA and 30 mg of PEG-PLGA-PEG in a mixed solvent of 2 ml of acetone and dichloromethane (acetone:dichloromethane = 1:8) as the oil phase, and prepare a mass fraction of 0.5% The PVA solution is used as the inner water phase;

[0041] (2) Under the condition of stirring in an ice-water bath, use a syringe to draw 30 μL of the inner aqueous phase in step (1) and drop it into the organic phase at a speed of 10-30 drops / min, ultrasonic for 5 s, intermittent for 5 s, and continuous ultrasonic for 10 min the formation of colostrum;

[0042] (3) Under the condition of stirring in an ice-water bath, draw the colostrum in step (2) with a syringe, and add it dropwise to 20 ml of 0.5% PVA solution at a speed of 10-30 drops / minute under the liquid surface Medium (the ratio of colostrum to double milk is 1:10), ultrasound for 5 s, intermittent 5 s, continuous ul...

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Abstract

The invention relates to tanshinone IIAPEG-PLGA-PEG (Tanshinone Polyethylene Glycol-Poly(Lactic-Co-Glycolic Acid)-Polyethylene Glycol) nanoparticles and preparation method thereof. An IIAPEG-PLGA-PEG triblock copolymer is adopted as a carrier material of the nanoparticles, a medicine, namely tanshinone IIA is loaded, the particle sizes of the nanoparticles range from 100nm to 400nm, the loading rate of the tanshinone IIA in the nanoparticles is 10-40%, the encapsulation efficiency is 50-90%, and the tanshinone IIAPEG-PLGA-PEG nanoparticles provided by the invention are simple in preparation process, uniform in size and smooth in surface. In addition, the loading rate and the encapsulation efficiency of medicines can be effectively improved, the hydrophilia, the biocompatibility and the bioavailability of the tanshinone IIA can be improved, medicine release can be effectively controlled, the circulation half-life periods of the medicines in bodies can be prolonged, and very important significances in treating cerebral arterial thrombosis and cardiovascular and cerebrovascular diseases can be achieved.

Description

technical field [0001] The invention relates to the field of medical technology, and relates to a preparation method and application of PEG-PLGA-PEG nanoparticles loaded with tanshinone IIA. Background technique [0002] Tanshinone IIA (Tanshinone IIA) is a diterpene quinone compound. It is one of the main active ingredients of Danshen, a traditional Chinese medicine for promoting blood circulation and removing blood stasis. It is a fat-soluble drug and is easily soluble in organic solvents. It is a natural antioxidant drug. Tanshinone IIA has a wide range of pharmacological effects. Tanshinone IIA can improve atherosclerosis by protecting vascular endothelial cells, reducing lipid peroxide in the body, and immune regulation. Clinical studies have found that tanshinone IIA also has the effect of inhibiting cardiomyocyte apoptosis, which plays a key role in the development of treatment of cardiovascular diseases; There are also significant therapeutic effects on central nerv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/58A61K47/34A61P9/10A61P9/00A61P25/28A61P29/00A61P39/06
CPCA61K31/58A61K9/5146
Inventor 刘欣李玉涛
Owner HARBIN UNIV OF SCI & TECH
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