Nano-carrier for tanshinone IIA and application thereof

A nano-carrier and tanshinone technology, applied in the field of biomedicine, can solve problems such as lack of sustained release effect, increased number of administrations, and cytotoxicity, and achieve the effects of improving bioavailability, improving solubility, and reducing side effects

Active Publication Date: 2018-11-16
GUANGDONG HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the commonly used organic solvents when dissolving tanshinone IIA preparations include ethanol, ethylene glycol, etc., or surface active agents such as Tween 20, Tween 80, PEG, and PVP are added; but because these agents have certain irritation and cytotoxicity , and there are limitations in use: no sustained release effect, high dosage
[0006] Although adding organic reagents and surfactants can improve the solubility of tanshinone IIA, when used as an intravenous injection, there are limitations in use because these reagents have certain irritation and cytotoxicity, and at the same time, the addition of these substances does not have sustained release effect, there will be an increase in the number of doses

Method used

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  • Nano-carrier for tanshinone IIA and application thereof
  • Nano-carrier for tanshinone IIA and application thereof
  • Nano-carrier for tanshinone IIA and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] This embodiment provides a method for synthesizing nanocarriers, which includes the following steps in turn:

[0044] S1) Dissolve 1 part of L-lactide, 1 part of polyethylene glycol monoether and 0.1 part of stannous isooctanoate in dichloromethane, and react at 100°C for 48 hours; after the reaction, precipitate 3 times in glacial ether, and then vacuum drying at 40°C for 3 days to obtain mPEG-PLA-OH; in step S1), the solid-liquid ratio of the L-lactide to the methylene chloride is 0.72g / mL, and the mPEG-PLA-OH The structural formula is:

[0045]

[0046] Among them, y≥2;

[0047] S2) Dissolve 1 part of mPEG-PLA-OH, 1 part of succinic anhydride and 0.5 part of 4-dimethylaminopyridine in chloroform, mix well and add triethylamine; after reacting at room temperature for 3 days, precipitate in ether for 3 times, and filtered; after filtering, vacuum-dried at 40°C for 3 days to obtain mPEG-PLA-COOH; in step S2), the solid-liquid ratio of the mPEG-PLA-OH to the chlorof...

Embodiment 2

[0053] This embodiment provides a method for synthesizing nanocarriers, which includes the following steps in turn:

[0054] S1) Dissolve 14.4 parts of L-lactide, 7.6 parts of polyethylene glycol monoether and 0.2 part of stannous isooctanoate in dichloromethane, and react at 130°C for 18 hours; after the reaction, precipitate in glacial ether for 3 times, and then vacuum drying at 40°C for 3 days to obtain mPEG-PLA-OH; in step S1), the solid-liquid ratio of the L-lactide to the methylene chloride is 0.72 g / mL of the mPEG-PLA-OH The structural formula is:

[0055]

[0056] Among them, y≥2;

[0057] S2) Dissolve 10 parts of mPEG-PLA-OH, 2 parts of succinic anhydride and 1.2 parts of 4-dimethylaminopyridine in chloroform, mix well and add triethylamine; after reacting at room temperature for 3 days, precipitate in ether and filter ; After filtration, vacuum-dry at 40°C for 3 days to obtain mPEG-PLA-COOH; in step S2), the solid-liquid ratio of the mPEG-PLA-OH to the chlorofo...

Embodiment 3

[0063] This embodiment provides a method for synthesizing nanocarriers, which includes the following steps in turn:

[0064] S1) Dissolve 50 parts of L-lactide, 40 parts of polyethylene glycol monoether and 10 parts of stannous isooctanoate in dichloromethane, and react at 160°C for 2 hours; after the reaction, precipitate 3 times in ice ether, and then vacuum drying at 40°C for 3 days to obtain mPEG-PLA-OH; in step S1), the solid-liquid ratio of the L-lactide to the methylene chloride is 0.72 g / mL of the mPEG-PLA-OH The structural formula is:

[0065]

[0066] Among them, y≥2;

[0067] S2) Dissolve 30 parts of mPEG-PLA-OH, 10 parts of succinic anhydride and 10 parts of 4-dimethylaminopyridine in chloroform, mix well and add triethylamine; after reacting at room temperature for 3 days, precipitate in ether and filter ; After filtration, vacuum-dry at 40°C for 3 days to obtain mPEG-PLA-COOH; in step S2), the solid-liquid ratio of the mPEG-PLA-OH to the chloroform is 0.1 g / ...

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Abstract

The invention discloses a nano-carrier for tanshinone IIA and application thereof, which belong to the technical field of biological medicines. The nano-carrier is methoxy polyethylene glycol-polylactic acid-tocopheryl polyethylene glycol 1000 succinate copolymer (mPEG-PLA-TPGS) or medicinal acid addition salt; and materials for the synthesis of mPEG-PLA-TPGS include L-lactide, methoxypolyethyleneglycol, succinic anhydride and tocopheryl polyethylene glycol 1000 succinate. The nano-carrier prepared by the invention can improve the solubility of tanshinone IIA in water, increase the bioavailability of tanshinone IIA, reduce the dosage of medicine and reduces toxic and side effects and irritation.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a nano-carrier of tanshinone IIA and its application. Background technique [0002] Cardiovascular disease is the number one killer that seriously endangers human health in the world today. It has the characteristics of "high incidence, high recurrence rate, high disability rate and high mortality rate" and "many complications". Governments and pharmaceutical industries all over the world attach great importance to the research and development of drugs for the prevention and treatment of cardiovascular diseases. At present, domestic cardiovascular disease drugs are divided into two categories: chemical drugs and traditional Chinese medicines. In the past, the main treatment drugs were nitrates, β-blockers and calcium preparations. Because cardiovascular diseases require long-term medication, and the long-term application of chemically synthesized drugs will caus...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K31/58A61K9/50A61P9/00A61P9/10C08G63/91C08G63/664C08G81/00
CPCA61K9/5031A61K31/58A61K47/34A61P9/00A61P9/10C08G63/664C08G63/912C08G81/00
Inventor 张敏州王磊毛帅
Owner GUANGDONG HOSPITAL OF TRADITIONAL CHINESE MEDICINE
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