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Polymer material containing cholic acid and liposome modified by same

A technology of polymer materials and liposomes, which is applied in the direction of liposome delivery, antineoplastic drugs, drug combinations, etc., can solve the problems of poor storage stability, no relevant literature reports, and large irritation, and achieve good biophase Capacitive, avoid non-specific adsorption, easy to scale up the effect of production

Inactive Publication Date: 2015-12-09
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, nanoemulsions contain a large amount of co-surfactants ethanol and propylene glycol, which are highly irritating and have poor storage stability.
[0007] At present, the technology of synthesizing oral liver targeting materials and preparing liposome drug delivery system with oral active liver targeting has not been reported in the relevant literature

Method used

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  • Polymer material containing cholic acid and liposome modified by same
  • Polymer material containing cholic acid and liposome modified by same
  • Polymer material containing cholic acid and liposome modified by same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] The synthesis of embodiment 1 cholic acid polymer material

[0052] Weigh 25 mg of cholic acid and dissolve it in 4 mL of N, N-dimethylformamide (DMF), add 14 mg of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC.HCL) , 10 mg of 1-hydroxybenzotriazole (HOBT) and 0.37 mg of 4-dimethylaminopyridine (DMAP), reacted at room temperature for 1 h. Weigh 90mgDSPE-PEG 2000 -NH 2 Dissolve in 4 mL of dichloromethane (DCM), slowly add the DCM liquid into the DMF liquid, and react at room temperature for 48 h. Add water to the reaction system to terminate the reaction.

Embodiment 2

[0053] The synthesis of embodiment 2 cholic acid macromolecule material

[0054] Weigh 8.7mg of cholic acid and dissolve it in 3mL of N,N-dimethylformamide (DMF), add 12.2436mg of 2-(7-azobenzotriazole)-N,N,N',N'-tetramethyl Urea hexafluorophosphate (HATU), weigh 40mg DSPE-PEG 2000 -NH 2 and 6.5 mg of triethylamine were dissolved in 3 mL of dichloromethane (DCM), and the DCM liquid was slowly added to the DMF liquid, and reacted at room temperature for 30 min. Add water to the reaction system to terminate the reaction.

Embodiment 3

[0055] Synthesis of embodiment 3 cholic acid macromolecule material

[0056] Weigh 25 mg of cholic acid and dissolve it in 4 mL of N, N-dimethylformamide (DMF), add 14 mg of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC.HCL) , 8.4mg of N-hydroxysuccinimide (NHS), reacted at room temperature for 4h. Weigh 90mgDSPE-PEG 2000 -NH 2 Dissolve in 4 mL of dichloromethane (DCM), slowly add the DCM liquid into the DMF liquid, and react at room temperature for 48 h. Add water to the reaction system to terminate the reaction.

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Abstract

The invention provides a polymer material, which is represented by the formula I and contains cholic acid, and a preparation method thereof. The invention further provides a liposome, which takes phosphatide and cholesterol as the carriers and is modified by the polymer material represented by the formula I. Drugs are coated in the phosphatide bi-molecule layer. The provided liposome has double functions of active targeting and passive targeting; and furthermore, the preparation method is simple and practical and can be applied to massive production. The in-vivo experiment results show that the liposome has a strong targeting performance on livers and thus has a good application prospect.

Description

technical field [0001] The invention relates to a cholic acid-containing polymer material and a modified liposome, belonging to the field of pharmaceutical preparations. Background technique [0002] For chronic diseases such as hepatitis, long-term injection of drugs will bring a lot of pain to patients. Oral administration is convenient and has many advantages such as better compliance. In order to achieve the desired curative effect, and the liver itself has the ability to tolerate the drug, the drug dose has little effect; large doses will undoubtedly seriously damage other organs and lead to organ failure. The oral liver-targeted drug delivery system can effectively deliver the drug to the lesion of the liver while reducing its systemic distribution, improving the therapeutic index of the drug and reducing adverse reactions, which has a positive role in promoting the treatment of liver diseases. Therefore, the development of oral liver-targeting pharmaceutical preparat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48A61K47/34A61K9/127A61K31/357A61P35/00
Inventor 朱春燕黎迎
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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