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Temperature-sensitive lipopeptide, liposome containing the lipopeptide and application thereof

A liposome and sensitive technology, applied in the field of physical chemistry, can solve the problems of enhanced drug side effects, increased drug leakage, etc.

Inactive Publication Date: 2017-04-12
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such as Gerben A.Koning [1] 、David Needham [2] etc. have mentioned in the literature that utilizing the difference in the phase transition temperature of various phospholipids to adjust the phase transition temperature Tm of liposomes by the composition ratio of phospholipids, although there is a certain effect of increasing the amount of release above its Tm, but When the temperature is lower than Tm, the leakage of the drug will increase accordingly, which will enhance the side effects of the drug. Therefore, some literatures also report the synthesis of thermosensitive block copolymers [3] , insert it into the liposome bilayer membrane, the temperature-controlled drug release effect of such liposomes is indeed improved, but there is also the problem of polymer degradation in vivo

Method used

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  • Temperature-sensitive lipopeptide, liposome containing the lipopeptide and application thereof
  • Temperature-sensitive lipopeptide, liposome containing the lipopeptide and application thereof
  • Temperature-sensitive lipopeptide, liposome containing the lipopeptide and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] The lipopeptide structure is [CH 3 -(CH 2 ) 6 Preparation of lipopeptide-liposomes of -VAQLEVK-VAQLESK-VSKLESK-VSSLESK]

[0082] Preparation of solution

[0083] 1. Preparation of phospholipid solution: Use an analytical balance to weigh 9.04mg HSPC, 9.72mg DSPC, and 0.85mgDPPE, add them together to a 5ml volumetric flask, and dissolve them in a mixed solvent of chloroform:methanol at a ratio of 4:1.

[0084] 2. Preparation of cationic cholesterol solution: use an analytical balance to weigh 3.3 mg of 3β-[N-(dimethylaminoethane) carbamoyl cholesterol, dissolve it in a mixed solvent of chloroform:methanol at a ratio of 4:1 and set the volume to 5ml in the bottle.

[0085] 3. Preparation of lipopeptide solution: Weigh 0.39 mg leucine zipper lipopeptide [CH 3 -(CH 2 ) 6 -VAQLEVK-VAQLESK-VSKLESK-VSSLESK], dissolved in methanol as a solvent and fixed to a 5ml volumetric flask.

[0086] 4. Preparation of buffer solution: take 75.875mg tris(hydroxymethyl)aminomethane...

Embodiment 2

[0101] The lipopeptide structure is [CH 3 -(CH 2 ) 4 Preparation of lipopeptide-liposomes of -VAQLEVK-VAQLESK-VSKLESK-VSSLESK]

[0102] Preparation of solution

[0103] 1. Preparation of phospholipid solution: Use an analytical balance to weigh 11.52mg DPPC, 12.4mg DSPC and 1.09mgDPPE, add them together to a 5ml volumetric flask, and dissolve to volume with a mixed solvent of chloroform:methanol at a ratio of 4:1.

[0104] 2. Preparation of cholesterol solution: Weigh 2.5 mg of cholesterol with an analytical balance, dissolve it in a mixed solvent of chloroform:methanol at a ratio of 4:1, and transfer it to a 5 ml volumetric flask.

[0105] 3. Preparation of lipopeptide solution: weigh 0.5 mg leucine zipper lipopeptide CH with an analytical balance 3 -(CH 2 ) 4 -VAQLEVK-VAQLESK-VSKLESK-VSSLESK, dissolved in methanol as a solvent and set to volume in a 5ml volumetric flask.

[0106] 4. Preparation of rhodamine solution: take 20 mg of rhodamine into a 10 ml volumetric f...

Embodiment 3

[0117] The lipopeptide structure is [CH 3 -(CH 2 ) 4 Preparation of lipopeptide-liposomes of -VAQLEVK-VAQLESK-VSKLESK-VSSLESK]

[0118] Preparation of solution

[0119] 1. Preparation of phospholipid solution: Use an analytical balance to weigh 11.52mg DPPC, 12.4mg DSPC and 1.09mgDPPE, add them together to a 5ml volumetric flask, and dissolve to volume with a mixed solvent of chloroform:methanol at a ratio of 4:1.

[0120] 2. Preparation of cholesterol solution: Weigh 2.5 mg of cholesterol with an analytical balance, dissolve it in a mixed solvent of chloroform:methanol at a ratio of 4:1, and transfer it to a 5 ml volumetric flask.

[0121] 3. Preparation of lipopeptide solution: weigh 0.5 mg leucine zipper lipopeptide CH with an analytical balance 3 -(CH 2 ) 4 -VAQLEVK-VAQLESK-VSKLESK-VSSLESK, dissolved in methanol as a solvent and set to volume in a 5ml volumetric flask.

[0122] 4. Preparation of rhodamine solution: take 20 mg of rhodamine into a 10 ml volumetric f...

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Abstract

The invention provides a temperature-sensitive lipopeptid, wherein a molecular structure of the lipopeptid is CH3-(CH2)n-(VXXLXXX)m; n is 4-10; m is 3-5; V is valine; L is leucine; and X is hydrophilic amino acid except for the valine and the leucine. The invention further provides a temperature-sensitive lipopeptid-lipidosome formed by self-assembly of lipopeptid and phospholipid at the molar ratio of (1-50) to 200. Through selecting different phospholipids, regulating and controlling the phospholipid ratio, adopting different lipopeptids and regulating and controlling the ratio of lipopeptids to phospholipids, the lipopeptid-lipidosome with different phase transition temperatures can be obtained, so that the target of targeted drug delivery is reached.

Description

technical field [0001] The invention belongs to the field of physical chemistry, and in particular relates to a synthetic temperature-sensitive lipopeptide and its application in liposomes. Background technique [0002] Liposome is a new type of pharmaceutical preparation, which uses vesicles formed by phospholipid bimolecular membranes to encapsulate drug molecules. Since the basic structure of the biological plasma membrane is also a phospholipid bimolecular membrane, liposomes have a structure similar to that of biological cells, so they have good biocompatibility. [0003] Among the various new liposomes studied, temperature-sensitive liposomes are a promising branch, which effectively utilizes the dual advantages of liposomes and thermotherapy to improve therapeutic effects and reduce side effects. Ordinary temperature-sensitive liposomes are generally composed of phospholipids and cholesterol. Each phospholipid has a specific phase transition temperature. Using phosph...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/16A61K9/127C07K14/00A61K47/24
Inventor 徐首红李炜王斯佳刘洪来
Owner EAST CHINA UNIV OF SCI & TECH
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