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Compound phospholipid thermosensitive lipidosome with effect of simultaneously delivering drugs in double target areas, preparation method and application thereof

A heat-sensitive liposome and complex phospholipid technology, which is applied in the field of pharmacy, can solve the problems of simultaneous drug delivery in multiple target areas, and achieve the effect of improving drug loading effect and stability, and enhancing anti-tumor effect

Active Publication Date: 2017-10-10
JINGCHU UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, inclusion complex liposome is a more efficient carrier, and can use lipid bilayer and internal water phase "dual drug loading", but it cannot achieve multi-target simultaneous drug delivery

Method used

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  • Compound phospholipid thermosensitive lipidosome with effect of simultaneously delivering drugs in double target areas, preparation method and application thereof
  • Compound phospholipid thermosensitive lipidosome with effect of simultaneously delivering drugs in double target areas, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Preparation of complex phospholipid thermosensitive liposomes with dual target area simultaneous drug delivery effect

[0034] 1) Take 1 part of folic acid, dissolve it in dimethyl sulfoxide, add 1.2 parts of N-hydroxysuccinimide (NHS) and 1.2 parts of N,N-dicyclohexylcarbodiimide (DCC), under nitrogen atmosphere Protected from light and magnetically stirred for 3 hours, add 1 part of amino-β-cyclodextrin dissolved in 8 ml of pyridine, continue stirring for 48 hours, and continue stirring for 2 hours at 45°C. Evaporate most of the solvent under reduced pressure, dissolve the obtained solid in 300ml of distilled water, let stand at 4°C for 12 hours, filter, evaporate the filtrate to 15ml under reduced pressure, add dropwise to 300ml of acetone, stir for 2 hours, take the precipitate, wash with acetone Then vacuum-dry overnight to obtain folic acid-modified cyclodextrin.

[0035] 2) Take curcumol and folic acid-modified cyclodextrin at a molar ratio of 1:1 to p...

Embodiment 2

[0037] Example 2 Preparation of complex phospholipid thermosensitive liposomes with dual target area simultaneous drug delivery effect

[0038] Referring to the preparation steps of Example 1, the difference from Example 1 is that the ratio of folic acid and amino β-cyclodextrin during synthesis is 1:2; the drug loaded is zedoary oil; the preparation of zedoary oil and folic acid modified cyclodextrin The ratio of the inclusion complex is 5:1; the ratio of the free curcuma oil in the liposome to the curcuma oil in the folic acid-modified cyclodextrin inclusion complex is 1:2.

Embodiment 3

[0039] Example 3 Preparation of complex phospholipid thermosensitive liposomes with dual target area simultaneous drug delivery effect

[0040]With reference to the preparation steps of Example 1, the difference from Example 1 is that the ratio of folic acid and amino β-cyclodextrin during synthesis is 0.2:1; the loaded drug is β-elemene; β-elemene and The ratio of folic acid modified cyclodextrin to prepare clathrate is 2:1; the ratio of free β-elemene in liposome to β-elemene in folic acid modified cyclodextrin inclusion compound is 1:5.

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Abstract

The invention relates to a compound phospholipid thermosensitive lipidosome with an effect of simultaneously delivering drugs in double target areas, a preparation method and an application thereof. According to the invention, a folic acid modified cyclodextrin loaded drug is used for preparing an inclusion compound, and then the folic acid modified cyclodextrin inclusion compound and free drugs are respectively loaded into an inner water phase and a lipid bilayer of a compound phospholipid thermosensitive lipidosome; in an antitumor application, the free drugs and the drug-loading folic acid modified cyclodextrin inclusion compound are triggered to release from the lipidosome on a target part in the manner of heating; the free drugs mainly act on the tumor extracellular mesenchyme; the folic acid modified cyclodextrin inclusion compound enters tumor cells in the manner of receptor-mediated active targeting drug delivery; the simultaneous drug delivery in the tumor stroma and tumor cell double target areas is finally realized; the optimal therapeutic effect is realized in the manner of flexibly adjusting the drug ratio in the free drugs and the folic acid modified cyclodextrin inclusion compound. The invention is especially suitable for the antitumor application of complex component or monomer component of the traditional Chinese medicine with multiple effects and has wide application prospect in the aspect of research on a novel antitumor drug delivery system.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to targeted preparations and a preparation method and application thereof, in particular to a composite phospholipid thermosensitive liposome with simultaneous drug delivery effects in dual target areas, and a preparation method and application thereof. Background technique [0002] Traditional Chinese medicine ingredients generally have pleiotropic effects, which lies in the "multi-target synergistic effect". These targets are often located in different target areas, and the requirements for drug dosage are often different between different target areas. Therefore, simultaneous delivery of drugs to multiple target areas is required. And the adjustment of drug delivery ratio can be realized between different target regions. [0003] Both liposomes and clathrates belong to the category of new formulation technologies, which can improve the effect of drug delivery. In recent years, the active t...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/69A61K36/9066A61K31/352A61K31/122A61K31/015A61P35/00
CPCA61K9/1277A61K31/015A61K31/122A61K31/352A61K36/9066
Inventor 杨希雄陈军顾薇彭佩
Owner JINGCHU UNIV OF TECH
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