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Hydrophobic peptide-modified long-circulation liposome drug delivery system for injection

A long-circulating liposome and hydrophobic technology, which is applied in the direction of liposome delivery, antineoplastic drugs, drug combination, etc., can solve the problem of poor ability to enter cells, and achieve improved therapeutic index, high-throughput screening, source of broad effect

Inactive Publication Date: 2013-11-20
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

One of the reasons is that the targets of most anti-tumor drugs are located in the cells, and the liposomes must transport the drugs into the cells to exert their efficacy, while the ordinary long-circulating liposomes have poor ability to enter the cells

Method used

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  • Hydrophobic peptide-modified long-circulation liposome drug delivery system for injection
  • Hydrophobic peptide-modified long-circulation liposome drug delivery system for injection
  • Hydrophobic peptide-modified long-circulation liposome drug delivery system for injection

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Embodiment 1, the synthesis of guiding compound

[0034] Take a certain molar ratio of DSPE-PEG-NHS and hydrophobic peptides (PFVYLI, VPTLQ, QLPVM, VTVLALGALAGVGVG, and PIEVCMYREP), use anhydrous DMF as a solvent, adjust the pH to about 8, react, use TLC to track the reaction, and use HPLC to quantify Measure unreacted ligand. After the reaction was completed, dialyzed and lyophilized, the structure of the targeting compound was confirmed using MALDI-TOF to obtain DSPE-PEG-PFVYLI, DSPE-PEG-VPTLQ, DSPE-PEG-QLPVM, DSPE-PEG-VTVLALGALAGVGVG and DSPE-PEG-PIEVCMYREP.

Embodiment 2

[0035] Embodiment 2, the synthesis of guiding compound

[0036] After epoxidizing the double bond in cyclosporine A (CsA), it reacts with ethylenediamine to obtain aminated cyclosporine A. Take a certain molar ratio of NHS-PEG-DSPE and aminated cyclosporin A, use anhydrous DMF as a solvent, adjust the pH to about 8, react, use TLC to track the reaction, and use HPLC to quantitatively measure the unreacted ligand. After the reaction was completed, dialyzed and freeze-dried, the structure of the targeting compound was confirmed using MALDI-TOF to obtain DSPE-PEG-CsA.

Embodiment 3

[0037] Embodiment 3, the cyclosporin A modified long circulation liposome of encapsulating doxorubicin

[0038] Doxorubicin is a commonly used anti-tumor drug, and its target is located in the nucleus, which is a substrate of P-gp. Take lecithin, cholesterol, DSPE-PEG, DSPE-PEG-CsA (mass ratio: 10:2.5:1.8:1), put them in an eggplant-shaped bottle and add appropriate amount of chloroform to dissolve them. Rotary evaporation under reduced pressure at 40°C formed a uniform transparent film. Add 123mM ammonium sulfate solution, and sonicate in a water bath until blue opalescence appears. The obtained liposomes were repeatedly squeezed through a 0.2 μm polycarbonate membrane, and the prepared blank liposomes were passed through a Sephadex column, eluted with PBS (pH 7.4) buffer, and the liposome fraction was collected. Preheat the liposomes in a water bath at 40°C for a while, add an appropriate amount of adriamycin aqueous solution (2 mg / ml), place on an air shaker at 40°C for 2...

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Abstract

The invention belongs to a dosage form and preparation technology field, and relates to a anticancer medicament-carried targeting long circulating liposome drug delivery system for injection, which is characterized in that the long circulating liposome is modified by hydrophobic peptides. Wherein, the hydrophobic peptides has strong endophilicity with a cell membrane, and can be inserted into the cell membrane by hydrophobic effect, and the hydrophobic peptide-modified long-circulation liposome provided by the invention can increase capability of the liposome in a tumor tissue to permeate a tumor cell membrane, so as that a carried medicament can reach a target in a cell, thereby raising curative effect of an anticancer medicament. The hydrophobic peptide-modified long-circulation liposome drug delivery system for injection is characterized in that: by a membrane inserting function, the hydrophobic peptides are modified on the surface of the long circulating liposome, in order to increase transhipment of the anticancer medicament in the tumor cells.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical dosage forms and preparations, and relates to a hydrophobic peptide-modified long liposome delivery system loaded with anticancer drugs for injection, which is used for increasing the intratumoral transport of anticancer drugs. Background technique [0002] Malignant tumors are one of the main causes of human death. As the world's population ages, the number of cancer deaths worldwide is projected to continue to rise. At present, the treatment of malignant tumors is still a major problem facing medicine. Drug chemotherapy is the most commonly used method in clinical treatment of malignant tumors. However, most chemotherapeutic drugs are non-selective. While killing tumor cells, they also have a killing effect on normal cells, resulting in serious toxic side effects, such as the cardiotoxic effect of doxorubicin. The use of nano-carriers (such as liposomes, nanoparticles, micelles, etc.) ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/42A61P35/00
Inventor 张强代文兵高薇蔡德富
Owner PEKING UNIV
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