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Galactose ester modified traditional Chinese and western medicine jointly-loaded orally-taking liver-targeting microemulsion delivery system

A delivery system, lactose ester technology, applied in emulsion delivery, anti-tumor drugs, drug combination and other directions, can solve the problems of full attention to physical and chemical properties, achieve enhanced oral absorption and availability, enhance tissue specificity, and reduce tissue and organ damage Effect

Inactive Publication Date: 2015-12-23
JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the current studies on polysaccharides from traditional Chinese medicine plants only focus on their pharmacological activities, and their unique physical and chemical properties have not yet been fully paid attention to by the field of pharmacy.

Method used

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  • Galactose ester modified traditional Chinese and western medicine jointly-loaded orally-taking liver-targeting microemulsion delivery system
  • Galactose ester modified traditional Chinese and western medicine jointly-loaded orally-taking liver-targeting microemulsion delivery system
  • Galactose ester modified traditional Chinese and western medicine jointly-loaded orally-taking liver-targeting microemulsion delivery system

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Octanoylgalactosyl ester based on the principle of hydrophobic bond integration was used as the tumor targeting ligand, the anti-tumor drug vincristine with strong hydrophobic ability was used as the model drug, coix seed oil was used as the oil phase, RH40 was used as the emulsifier, and PEG400 was used as the model drug. Co-emulsifier, prepared microemulsion by water drop method. The specific method is as follows:

[0033] Take 150-200mg of RH40 and 20-35mg of capryloyl galactose ester and add it to 50-66mg of PEG400, stir magnetically at room temperature for 2-4 hours until completely mixed, and set aside; take 200-300mg of coix seed oil and 2-5mg of vincristine In the prepared mixed system, magnetically stir at room temperature for 2-4 hours until it is evenly mixed, and set aside; mix 150-300 mg coix seed polysaccharide into the water phase to form a coix seed polysaccharide aqueous solution, and then drop the coix seed polysaccharide aqueous solution at a constant...

Embodiment 2

[0035] 4-(6'-galactose)-1-benzylsuccinyl ester based on the principle of π-π stacking integration is used as the tumor targeting ligand, and paclitaxel, an anti-tumor drug containing more aromatic rings, is used as the model drug. Coix seed oil was used as oil phase, RH40 was used as emulsifier, PEG400 was used as co-emulsifier, and microemulsion was prepared by water drop method. The specific method is as follows:

[0036] Take 150~200mg of RH40 and 20~35mg of 4-(6'-galactose)-1-benzylsuccinyl ester, add it to 50~66mg of PEG400, stir magnetically at room temperature for 2~4 hours until completely mixed, and set aside; take 200~300mg of coix coix Add kernel oil and 2-5 mg of paclitaxel to the mixed system prepared above, stir magnetically at room temperature for 2-4 hours until well mixed, and set aside; mix 150-300 mg of coix seed polysaccharide into the water phase to form a coix seed polysaccharide aqueous solution, and then mix the coix seed polysaccharide aqueous solution...

Embodiment 3

[0038] The polylysine galactosyl ester based on the principle of hydrogen bond interaction was used as the tumor targeting ligand, the antineoplastic drug cisplatin containing more hydrogen bond donors / acceptors was used as the model drug, and coix seed oil was used as the oil phase , RH40 is an emulsifier, PEG400 is a co-emulsifier, and the microemulsion is prepared by water drop method. The specific method is as follows:

[0039] Add 150-200mg RH40 and 20-35mg polylysine galactosyl ester to 50-66mg PEG400, stir magnetically at room temperature for 2-4 hours until completely mixed, and set aside; take 200-300mg coix seed oil and 2-5mg cisplatin In the mixed system prepared above, stir magnetically at room temperature for 2-4 hours until it is evenly mixed, and set aside; mix 150-300 mg of coix seed polysaccharide into the water phase to form a coix seed polysaccharide aqueous solution, and then slowly and quantitatively drop the coix seed polysaccharide aqueous solution into ...

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Abstract

The invention discloses a galactose ester modified traditional Chinese and western medicine jointly-loaded orally-taking liver-targeting microemulsion delivery system and a preparation method and application thereof. Traditional Chinese medicine polysaccharide components and traditional Chinese medicine oil components with an antitumor effect are used as functional minor ingredients to construct microemulsion carriers, difficultly soluble antitumor drugs are embedded and galactose ester is adopted for modification. The system realizes the liver targeting of orally taking drugs, improves the tissue specificity of the drugs, improves the curative effect and reduces the damages to other tissues and organs; the system not only can be used for increasing the solubility of difficultly soluble components (traditional Chinese medicine oil and difficultly soluble antitumor drugs) and controlling dug release, but also can form nano-scale emulsion in water; the microemulsion medicinal components can obviously improve the oral taking absorption utilization degree by virtue of the in-vivo absorption characteristic of the nano emulsion; the dosage of conventional minor ingredients is greatly reduced, the drug loading capacity is improved and the in-vivo toxicity is reduced.

Description

technical field [0001] The present invention relates to a galactose ester-modified Chinese and Western medicine co-loaded oral liver-targeted microemulsion delivery system and the application of the microemulsion system in anti-liver cancer. The system is replaced by traditional Chinese medicine oils and polysaccharides with anti-tumor effects The microemulsion system of conventional oil phase and emulsifier auxiliary materials embeds insoluble anti-tumor chemotherapy drugs, and uses galactose esters as liver targeting ligands for modification. Background technique [0002] Traditional Chinese medicine nano drug delivery system is a hot research field in the modernization of traditional Chinese medicine preparations. As a kind of nano drug delivery system, microemulsion is formed by self-assembly of emulsifier, co-emulsifier and oil phase, which can significantly solubilize insoluble traditional Chinese medicine components, promote their oral absorption, and have passive liv...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/44A61K47/36A61K47/48A61K36/8994A61K36/185A61K36/9066A61K36/55A61K36/284A61K31/475A61K31/337A61K33/24A61K31/7048A61P35/00
Inventor 陈彦瞿鼎刘明健
Owner JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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