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Paclitaxel platinum co-loaded targeting long-circulating liposome and application thereof

A long-circulating liposome and paclitaxel technology, which is applied in the directions of liposome delivery, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve the problems of low encapsulation rate, non-targeting, and limited clinical application effect, etc. To improve the effect of targeted therapy, reduce capture interference, and improve the quality of life

Active Publication Date: 2021-04-16
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although platinum-based liposome drugs reduce the toxic and side effects of drugs to some extent in the process of tumor treatment, there are defects of low encapsulation efficiency and non-targeting in ordinary liposomes, which limit their use. Clinical application effect

Method used

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  • Paclitaxel platinum co-loaded targeting long-circulating liposome and application thereof
  • Paclitaxel platinum co-loaded targeting long-circulating liposome and application thereof
  • Paclitaxel platinum co-loaded targeting long-circulating liposome and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] A method for preparing paclitaxel-cisplatin co-loaded targeted long-circulation liposomes, comprising:

[0040] Weigh 60mg PC (yolk lecithin), 15mg Chol (cholesterol), 10.1mg PTX (Paclitaxel, paclitaxel) and 24.8mg mPEG 2000 -DSPE (methoxy-polyethylene glycol-distearoylphosphatidylethanolamine, purchased from Shanghai Xibao Biotechnology Co., Ltd.) was dissolved in 15mL chloroform solvent, the molar ratio PC:Chol=2:1, PTX:( (PC+Chol)=1:10, (PC+Chol):mPEG 2000 -DSPE=20:1.

[0041] Mix the above mixed solution at 50°C under normal pressure for 3 to 5 minutes to fully mix PTX and phospholipids, then slowly vacuumize at a speed of 100rpm and then spin evaporate the solvent. , then add 3.6mL of glucose solution containing cisplatin (the concentration of cisplatin is 1.9mg / mL, the ratio of drug to lipid is 1:5, that is, the molar ratio of cisplatin:PC+Chol), hydrate at 37°C for 2h, add 2.2mg ES-DSPE-PEG 2000 (dissolved with 0.2mL glucose solution) mixed and shaken gently,...

Embodiment 2

[0046] A method for preparing paclitaxel-oxaliplatin co-loaded targeted long-circulation liposomes, comprising:

[0047] A certain amount of hydrogenated soybean lecithin (HSPC), cholesterol, PTX and mPEG 2000 -DSPE is dissolved in 10mL chloroform solvent, in which the ratio of phospholipid to cholesterol is 4:1, and the ratio of drug to lipid is 1:20 (that is, the molar ratio of drug: HSPC+Chol), (HSPC+Chol):mPEG 2000 -DSPE=15:1.

[0048] Evaporate the above mixed solution to form a film under reduced pressure, then add dissolved oxaliplatin (OXA) and a small amount of ES-DSPE-PEG 2000 The 5% glucose solution of the fragment was hydrated at 37° C. for 2 hours (OXA concentration was 1 mg / mL), and the probe was ultrasonically cooled for 3 seconds in an ice-water bath for 3 seconds for a total of 10 minutes to obtain liposomes.

[0049] The above-mentioned liposomes were extruded three times through a liposome extruder through a polycarbonate 80nm membrane to obtain paclitaxel...

Embodiment 3

[0051] A method for preparing paclitaxel-carboplatin-co-loaded targeted long-circulation liposomes, comprising:

[0052]80mg egg yolk lecithin (EPC), 27.2mg cholesterol, 15mg PTX, 37mg mPEG 2000 -DSPE and 3.4mg ES-DSPE-PEG 2000 Dissolve in 10 mL of chloroform according to the molar ratio of 6:4:1:0.75:0.075.

[0053] Mix the above mixed solution under normal pressure for 3 to 5 minutes to fully mix PTX and phospholipids, then slowly evacuate the solvent and evaporate the solvent to make it dry quickly to a translucent film, then add 5.4 mL of carboplatin (CBP) 5% glucose solution (carboplatin concentration: 1.2mg / mL), molar ratio CBP:PTX=1:1, 37°C medium-speed rotation to hydrate the film for 1h. Then, the probe was ultrasonically cooled for 3 seconds in an ice-water bath for 3 seconds for a total of 10 minutes, and extruded three times through a liposome extruder through a polycarbonate 80 nm membrane to obtain paclitaxel-carboplatin long-acting targeted co-loaded liposomes...

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Abstract

The invention discloses a paclitaxel and platinum co-loaded targeting long-circulating liposome and application thereof. The liposome is formed by reacting paclitaxel, platinum drugs, a DSPE-G2000-ES targeting fragment, an mPEG2000-DSPE long-acting fragment, lecithin and cholesterol; wherein the platinum medicine is prepared from any one of cis-platinum, oxaliplatin and carboplatin. According to the paclitaxel platinum co-loaded targeting long-circulating liposome, a targeting fragment is used as a fragment for specifically recognizing an estrogen receptor, specifically recognizes and is combined with the estrogen receptor on the surface of an SKOV3 cell, so that the ingestion of the liposome is increased; the long-acting fragment reduces the capture interference of the liposome with albumin and reticuloendothelial systems in vivo, and prolongs the circulation time of the liposome in vivo; the IC50 value of the liposome to SKOV3 cells is 0.20-0.23 [mu]M, the tumor inhibition rate is 65-90%, and the liposome has a very good anti-ovarian cancer effect.

Description

technical field [0001] The invention relates to a co-loaded targeted long-circulation liposome, in particular to a paclitaxel-platinum co-loaded targeted long-circulated liposome and its application for targeting estrogen receptors. Background technique [0002] Carcinoma refers to malignant tumors originating from epithelial tissue, and is the most common type of malignant tumors. Ovarian cancer is the leading cause of cancer death in women and the fifth leading cause of death in women worldwide. It is prone to recurrence and has a poor prognosis. The five-year survival rate in Europe is between 26% and 51%. Because the early stages of ovarian cancer seldom cause any symptoms and due to the special anatomical location of women, more than 70% of ovarian cancer patients have entered the advanced stage of cancer (that is, stage III or IV) when they first see the doctor, and the advanced stage Ovarian cancer may cause non-specific symptoms, and the mortality rate of ovarian ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61K31/555A61K33/243A61P35/00
Inventor 裴瑾唐欢任智慧贾娟李倩文陈虹羽吕哲包涵朱明谢一卓张燕刘蕊沈雨佳郑玉翠
Owner JILIN UNIV
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