High-polymer material with cholic acid and liposome modified by high-polymer material

A technology of polymer materials and liposomes, which can be applied in the directions of liposome delivery, medical preparations of inactive ingredients, and digestive systems, etc., can solve the problems of poor storage stability, no relevant literature reports, and high irritation, etc. Achieve good biocompatibility, avoid non-specific adsorption, and easily scale up production

Active Publication Date: 2018-06-12
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.
[0008] 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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  • High-polymer material with cholic acid and liposome modified by high-polymer material
  • High-polymer material with cholic acid and liposome modified by high-polymer material
  • High-polymer material with cholic acid and liposome modified by high-polymer material

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The synthesis of embodiment 1 cholic acid polymer material

[0053] 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 1-hydroxybenzotriazole (HOBT) and 0.37 mg 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

[0054] The synthesis of embodiment 2 cholic acid macromolecule material

[0055] 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'- Tetramethyluronium 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

[0056] Synthesis of embodiment 3 cholic acid macromolecule material

[0057] 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 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 high-polymer material with cholic acid, a method for preparing the high-polymer material and liposome. The high-polymer material is shown as a formula I. Phospholipid and cholesterol are used as carriers for the liposome, the liposome is modified by the high-polymer material shown as the formula I, and medicines are entrapped in bi-molecular layers of the phospholipid. Thehigh-polymer material, the method and the liposome have the advantages that an active targeting effect and a passive targeting effect can be realized by the liposome; the method is simple and practical, amplification production can be facilitated, the high-polymer material and the liposome are high in targeting capacity for livers as shown in in-vivo experiments, and accordingly the high-polymermaterial, the method and the liposome have excellent application prospects.

Description

[0001] This application is a divisional application of a patent application with the application number 201510468166.0, the application date is August 3, 2015, and the invention title is "a polymer material containing cholic acid and its modified liposome". technical field [0002] The invention relates to a cholic acid-containing polymer material and a modified liposome, belonging to the field of pharmaceutical preparations. Background technique [0003] 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/332A61K47/28A61K47/24A61K9/127A61P1/16A61P31/14A61P31/20
Inventor 朱春燕黎迎
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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