Preparation method and application of targeted multi-function double drug-loading liposome

A multifunctional, targeting phospholipid technology, applied in the direction of liposome delivery, preparations for in vivo testing, pharmaceutical formulations, etc., can solve problems such as toxicity and neurotoxicity, non-targeting, allergic reactions, etc., to achieve enhanced effect effect, improving efficacy, reducing side effects

Active Publication Date: 2015-04-08
INNOVATION ACAD FOR PRECISION MEASUREMENT SCI & TECH CAS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation can cause many side effects, such as allergic reactions, nephrotoxicity and neurotoxicity, etc.
[0005] In clinical practice, paclitaxel and platinum drugs are often used in combination

Method used

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  • Preparation method and application of targeted multi-function double drug-loading liposome
  • Preparation method and application of targeted multi-function double drug-loading liposome
  • Preparation method and application of targeted multi-function double drug-loading liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1: Preparation of targeted multifunctional dual drug-loaded liposomes (RGD-CPGd-L)

[0057] The raw material components include: basic membrane material phospholipids (distearoylphosphatidylcholine and distearoylphosphatidylglycerol), PEG-modified phospholipid MPEG-2000-DSPE, targeting phospholipid RGD cyclic peptide-polyethylene glycol 2000- Distearoylphosphatidylethanolamine, paclitaxel, carboplatin, gadolinium diamine.

[0058] The molar ratio of each component is as follows:

[0059] Distearoylphosphatidylcholine: Distearoylphosphatidylglycerol: MPEG-2000-DSPE: RGD cyclic peptide-polyethylene glycol 2000-distearoylphosphatidylethanolamine=7:2:1:0.5.

[0060] The basic membrane material phospholipid: Paclitaxel = 30:1.

[0061] The basic membrane material phospholipid: carboplatin = 2:1.

[0062] The basic membrane material phospholipid: Gadolinium diamine=1:5000.

[0063] The molar amount of the basic membrane material phospholipid refers to the sum of the molar amount...

Embodiment 2

[0067] The fluorescent targeting multifunctional dual drug-loaded liposome (Rh-RGD-CPGd-L) was prepared with reference to the method of Example 1. The difference from Example 1 is that nordamine-bismyristylphosphatidylethanolamine was added to the raw material (Rhod-DMPE), the molar ratio of this component to other phospholipids is: distearoylphosphatidylcholine: distearoylphosphatidylglycerol: MPEG-2000-DSPE: RGD cyclic peptide-polyethylene glycol 2000-dihard Fatty acylphosphatidylethanolamine: Rhod-DMPE=7:2:1:0.5:0.2. During the preparation process, Rhod-DMPE, PEG modified phospholipid and targeted phospholipid are added together.

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Abstract

The invention belongs to the preparation and application technical field of the liposome and specifically discloses a preparation method and application of targeted multi-function double drug-loading liposome. The raw material for the targeted multi-function double drug-loading liposome comprises the basic film material phospholipid, polyethylene glycol modified phospholipid capable of prolonging the half-life period of the liposome medicine blood, phospholipid capable of having fluorescence imaging, phospholipid having targeted function, lipid-soluble drug and water-soluble drug treating the tumor and contrast agent capable of strengthening nuclear magnetism imaging signal. The medicine can solve the clinic use defect of the medicine with poor water solubility through the package of the phospholipid, the method of administration of the conventional medicine is changed by combining with the water-soluble drug, the targeting action is achieved for the tumor tissue for effectively restraining the tumor growth, reducing the production of the side reaction; the medicine action effect and the tumor change condition can be observed in real time through MRI and great clinical application value is achieved.

Description

Technical field [0001] The invention relates to the technical field of preparation and application of liposomes, and more particularly to a preparation method and application of a targeted multifunctional dual drug-loaded liposome. Background technique [0002] Liposomes composed of phospholipids are similar in composition and structure to biological cell membranes and have good biocompatibility. Liposomes contain a phospholipid bilayer and a hydrophilic core region, which can carry water-soluble and fat-soluble substances, which can improve many deficiencies in drug application. As a drug carrier, liposomes have been successfully used to carry various drugs. Including doxorubicin, cathepsin inhibitors, irinotecan, vinorelbine and osmanthus, diclofenac sodium, etc. [0003] Platinum drugs, including cisplatin, carboplatin, oxaliplatin, etc., can bind to DNA and hinder DNA replication and RNA translation, thereby promoting tumor cell death. It is often used in various cancer trea...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K45/06A61K47/34A61K49/00A61K49/18A61P35/00
Inventor 周欣任莉莉陈世桢孙献平刘买利
Owner INNOVATION ACAD FOR PRECISION MEASUREMENT SCI & TECH CAS
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