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Targeted long-circulation liposome based on mim protein cyclic peptide inhibitor and its preparation method and application

A long-circulating liposome and cyclic peptide inhibitor technology, which is applied in liposome delivery, cyclic peptide components, pharmaceutical formulations, etc., can solve the problems of increasing drug therapeutic index, improve tumor treatment effect, reduce toxic and side effects, selective effect

Active Publication Date: 2017-01-11
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Anticancer drugs encapsulated in long-circulating liposomes can significantly increase the therapeutic effect of anticancer drugs through passive targeting, but selective targeting to the site of action in the body will further increase the therapeutic index of the drug than passive targeting

Method used

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  • Targeted long-circulation liposome based on mim protein cyclic peptide inhibitor and its preparation method and application
  • Targeted long-circulation liposome based on mim protein cyclic peptide inhibitor and its preparation method and application
  • Targeted long-circulation liposome based on mim protein cyclic peptide inhibitor and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The preparation of the targeted long circulation liposome based on MIM protein cyclic peptide inhibitor comprises the following steps:

[0042] (1) Bis-p-nitrophenyl carbonate polyethylene glycol 2000 (pNP-PEG 2000 -pNP) preparation

[0043]

[0044] 5g polyethylene glycol 2000 (PEG 2000 ) was dissolved in 50mL of dichloromethane, then added 1mL of triethylamine and 1g of p-nitrophenyl chloroformate and stirred at room temperature for 12h. After the reaction was complete, precipitate and filter the triethylamine hydrochloride formed in the system , the filtrate was evaporated to dryness under reduced pressure, and the obtained crude product was recrystallized with ether and ethyl acetate, respectively, to finally obtain 3.6 g of a white powder product, which was bis-p-nitrophenyl carbonate polyethylene glycol 2000.

[0045] 1 H-NMR (500MHZ, CDCl 3 )δ (ppm): 3.59-3.68 (m, multi H, back bone–OCH 2 CH 2 O-),4.43(t,4H,-CH 2 OCO),7.35(d,4H,J=7.8Hz,Ar-H),8.19(d,4H,J...

Embodiment 2

[0055] The preparation of the targeted long circulation liposome based on MIM protein cyclic peptide inhibitor comprises the following steps:

[0056] (1) Bis-p-nitrophenyl carbonate polyethylene glycol 4000 (pNP-PEG 4000 -pNP) preparation

[0057] 5 g polyethylene glycol 4000 (PEG 4000 ) was dissolved in 50mL of dichloromethane, then added 1mL of triethylamine and 2g of p-nitrophenyl chloroformate and stirred at room temperature for 10h. After the reaction was complete, precipitate and filter the triethylamine hydrochloride formed in the system , the filtrate was evaporated to dryness under reduced pressure, and the obtained crude product was recrystallized with ether and ethyl acetate, respectively, to finally obtain 3.6 g of a white powder product, which was bis-p-nitrophenyl carbonate polyethylene glycol 4000.

[0058] (2) Distearoylphosphatidylethanolamine-polyethylene glycol 4000-p-nitrophenyl carbonate (DSPE-PEG 4000 -pNP) preparation

[0059] Bis-p-nitrophenyl carb...

Embodiment 3

[0063] The preparation of the targeted long circulation liposome based on MIM protein cyclic peptide inhibitor comprises the following steps:

[0064](1) Bis-p-nitrophenyl carbonate polyethylene glycol 6000 (pNP-PEG 6000 -pNP) preparation

[0065] 5g polyethylene glycol 6000 (PEG 6000 ) was dissolved in 50mL of dichloromethane, then 1mL of triethylamine and 3g of p-nitrophenyl chloroformate were added and stirred at room temperature for 15h. After the reaction was complete, the precipitated triethylamine hydrochloride formed in the system was filtered. , the filtrate was evaporated to dryness under reduced pressure, and the obtained crude product was recrystallized with ether and ethyl acetate, respectively, to finally obtain 3.6 g of a white powder product, which was bis-p-nitrophenyl carbonate polyethylene glycol 6000.

[0066] (2) Distearoylphosphatidylethanolamine-polyethylene glycol 6000-p-nitrophenyl carbonate (DSPE-PEG 6000 -pNP) preparation

[0067] The bis-p-nitro...

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Abstract

The invention provides targeted long-circulating liposome based on an MIM (Metal injection Molding) protein cyclopeptide inhibitor. The targeted long-circulating liposome is characterized in that the structural formula is shown as formula (I) described in the specification. The invention also provides a preparation method of the targeted long-circulating liposome based on the MIM protein cyclopeptide inhibitor, and an application of the targeted long-circulating liposome based on the MIM protein cyclopeptide inhibitor in preparation of antineoplastic drugs. The liposome is high in selectivity and high in safety, realizes targeted drug delivery for tumor cells, and also reduces the toxic and side effects of antitumor drugs; in addition, a micromolecular cyclopeptide inhibitor S3-a02 can coordinate with other liposome-cladding antineoplastic drugs to play double efficacy, and thus the tumor treatment effect can be greatly improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical polymer excipients, and in particular relates to a targeted long-circulation liposome based on MIM protein cyclic peptide inhibitor, which is a cyclic peptide inhibitor based on MIM protein I-BAR dimer S3-a02 is a polyethylene glycol-modified phospholipid derivative targeting a ligand, and also relates to the application of the liposome in the preparation of antitumor drugs. Background technique [0002] Liposome is a molecular orderly assembly spontaneously formed by phospholipids in water by means of hydrophobic association. The water phase and the oil phase between the bimolecular membranes. Its properties are similar to cell membranes, so it has good biocompatibility. However, when liposomes enter the blood circulation system, they are easily recognized by the reticulo-endothelial system (RES) and quickly leave the blood stream. Therefore, "long circulation" is the basic property that liposome...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/42A61K9/127A61K31/704A61K31/337A61K31/352A61K31/475A61K38/13A61P35/00
Inventor 蔡进吉民曹萌陈峻青
Owner SOUTHEAST UNIV
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