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Tumor targeted lipidosome drug-delivering system, preparation method and application

A drug delivery system and tumor targeting technology, applied in the field of polypeptide-modified active targeting liposome drug delivery system, can solve the problems of limited application, cytotoxicity, system stability reduction, etc., achieve good curative effect, prolong median effect of survival

Inactive Publication Date: 2016-12-14
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the targeting group is modified on the surface of nanoparticles and enters the body circulation, the stability of the system is reduced, and there is certain cytotoxicity after drug loading, so its application in treatment is limited.

Method used

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  • Tumor targeted lipidosome drug-delivering system, preparation method and application
  • Tumor targeted lipidosome drug-delivering system, preparation method and application
  • Tumor targeted lipidosome drug-delivering system, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Synthesis, Purification and Characterization of CRNGRGPDC--PEG--DSPE

[0034] Dissolve CRNGRGPDC in PBS solution (pH7.4), dissolve maleimide-polyethylene glycol-phospholipid complex (Mal-PEG-DSPE) in DMF, mix the two and react with magnetic stirring, high performance liquid phase The reaction was monitored by chromatography (HPLC), and the reaction was stopped after the Mal-PEG-DSPE reaction was complete, and excess CRNGRGPDC and DMF were removed by dialysis (molecular weight cut-off 3.5kDa). After lyophilization, CRNGRGPDC-PEG-DSPE was obtained, and its structure was characterized by HPLC. The HPLC collection of illustrative plates shows that A figure is the HPLC collection of collection of Mal-PEG-DSPE, and B is the HPLC collection of collection of CRNGRGPDC-PEG-DSPE, and main peak retention time is by figure 2 The 27min of the picture A in the middle moves to about 20min of the picture B; the NMR spectrum shows that A is the NMR spectrum of Mal-PEG-DSPE, and B is the...

Embodiment 2

[0036] Preparation and Characterization of CRNGRGPDC--Liposome / DOX

[0037] The liposome composition is HSPC (hydrogenated soybean phospholipid) / Chol (cholesterol) / mPEG-DSPE (polyethylene glycol-distearoylphosphatidylethanolamine complex) (56:44:2, mol / mol), modified by CRNGRGPDC The PEG liposome membrane material formulation is HSPC / Chol / mPEG-DSPE / CRNGRGPDC-PEG-DSPE (56:44:2:1, mol / mol). The above-mentioned membrane material was weighed and dissolved in 1-4ml chloroform (analytical pure), and the organic solvent was removed by rotary evaporation under reduced pressure to obtain a uniform lipid membrane, which was dried in vacuum for 24 hours. Add ammonium sulfate aqueous solution for hydration, and shake in a water bath at 60°C for 2 hours to obtain a liposome suspension. In a water bath at 60°C, use a high-pressure homogenizer (if the liposome volume is less than 10 mL, use a micro extruder) to sequentially squeeze the liposomes through 400, 200, 100 and 50 nm nuclear pore ...

Embodiment 3

[0039] CRNGRGPDC--Preparation and Characterization of Liposome / FAM

[0040] The liposome formulation is composed of HSPC (hydrogenated soybean lecithin) / Chol (cholesterol) / mPEG-DSPE (polyethylene glycol-distearoylphosphatidylethanolamine complex) (56:44:2, mol / mol), CRNGRGPDC The modified PEG liposome membrane material was formulated as HSPC / Chol / mPEG-DSPE / CRNGRGPDC-PEG-DSPE (56:44:2:1, mol / mol). The above-mentioned membrane material was weighed and dissolved in 1-4ml chloroform (analytical pure), and the organic solvent was removed by rotary evaporation under reduced pressure to obtain a uniform lipid membrane, which was dried in vacuum for 24 hours. Add FAM aqueous solution for hydration, and shake in a water bath at 60°C for 2 hours to obtain a liposome suspension. In a water bath at 60°C, use a high-pressure homogenizer (if the liposome volume is less than 10 mL, use a micro extruder) to sequentially squeeze the liposomes through 400, 200, 100 and 50 nm nuclear pore membr...

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Abstract

The invention discloses a tumor targeted lipidosome drug-delivering system, a preparation method and an application. The system comprises a CRNGRGPDC polypeptide modified invisible lipidosome and an antitumor drug, wherein the invisible lipidosome comprises a) hydrogenated soyabean lecithin, b) cholesterol, c) polyethylene glycol-distearoyl phosphatidylethanolamine and d) distearoyl phosphatidylethanolamine-polyethylene glycol-CRNGRGPDC; the mole ratio of the components are as follows: a:b=(5-1):(1-5), a:c=1000:(0.1-100) and a:d=1000:(0.1-100); adriamycin amycin or pharmorubicin is taken as the antitumor drug; the weight percentage of the invisible lipidosome in the system is 75%-98%; the balance is the antitumor drug. The CRNGRGPDC provided by the invention is a cyclic peptide, is taken as aglucon and has pathoklisis with tumor cells. The invention also discloses the preparation method for the polypeptide modified lipidosome containing CRNGRGPDC sequence. The prepared polypeptide modified lipidosome containing CRNGRGPDC sequence is used for intravenous injection and is targeted to the tumor under the tumor EPR effect and CRNGRGPDC mediation. The lipidosome drug-delivering system can be used for targeting and delivering the drugs for tumor diagnosis or treatment.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a polypeptide-modified targeting liposome drug delivery system, in particular to a polypeptide-modified active targeting liposome drug delivery system containing a CRNGRGPDC sequence, a preparation method and its clinical application. Background technique [0002] Primary brain tumors in tumors have become a difficult problem in medicine. In the past 30 years, the incidence of primary malignant brain tumors has been increasing year by year, with an annual growth rate of about 1.2%. Patient survival rate is low. According to WHO statistics, the average survival time of patients with grade 4 glioma is only 12 months. As an intracranial tumor, glioma has many unique features, and its tumor formation and development have various barriers. , such as enzymatic barriers, the blood-brain barrier (BBB) ​​and the tumor blood-brain barrier (BBTB), hinder drugs or drug delivery syst...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/704A61K47/42A61P35/00
CPCA61K9/127A61K31/704A61K47/42
Inventor 俞磊周靖娥余静高礼鹏彭婷孙磊闫志强王镜朱建中王依婷
Owner EAST CHINA NORMAL UNIV
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