Molecular targeting drug-entrapped liposome and application of liposome in preparation of drug for treating tumors

A molecular targeting drug and targeting liposome technology, applied in the field of biomedicine, can solve problems such as affecting bioavailability, affecting curative effect, poor solubility, etc. effect, the effect of increasing flexibility

Inactive Publication Date: 2020-11-13
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Known multi-target inhibitors such as AL3180, sunitinib, regoratinib, sorafenib, vandetanib, cabozantinib, lenvatinib, pazopanib, vemurafenib , axitinib, dabrafenib, linivarib, nintedanib, etc.; some studies have reported that the poor solubility of most molecularly targeted drugs affects their bioavailability, or it is difficult to penetrate biological barriers (such as Blood-brain barrier BBB, blood-tumor barrier BTBB, etc.) affect its curative effect on brain tumors and some solid tumors

Method used

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  • Molecular targeting drug-entrapped liposome and application of liposome in preparation of drug for treating tumors
  • Molecular targeting drug-entrapped liposome and application of liposome in preparation of drug for treating tumors
  • Molecular targeting drug-entrapped liposome and application of liposome in preparation of drug for treating tumors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1, preparation and characterization of liposome / SCC-31 by active drug loading method

[0048] This example discloses the preparation and characterization of liposome / molecular targeting drug SCC-31 by the active drug loading method, which specifically includes the following steps:

[0049] The membrane material formulation of liposome / SCC-31 is HSPC / Chol / mPEG2000-DSPE (50:45:5, molar ratio). The above membrane materials were weighed and dissolved in chloroform, 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 a certain volume of 0.2M citric acid solution, and shake in a water bath at 60°C for 2 hours to obtain a liposome suspension. Ultrasonic cell pulverizer ultrasonicated for 10min (80w, ultrasonic 2s, interval 1s), and blank liposomes were obtained. Physiological saline was eluted and the blank liposome extracorporeal aqueous phase was replaced...

Embodiment 2

[0050] Embodiment 2, active drug loading method preparation D VAP-liposome / SCC-31 and its characterization

[0051] This example discloses the preparation of active drug loading method D VAP-liposome / molecular targeting drug SCC-31 and its characterization, specifically include the following steps:

[0052] D The formulation of VAP-liposome / SCC-31 membrane material is HSPC / Chol / mPEG 2000 -DSPE / D VAP-PEG 3400 - DSPE (50:45:3:2, molar ratio). The above membrane materials were weighed and dissolved in chloroform, 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 a certain volume of 0.2M citric acid solution, and shake in a water bath at 60°C for 2 hours to obtain a liposome suspension. Ultrasonic cell pulverizer ultrasonicated for 10min (80w, ultrasonic 2s, interval 1s), and blank liposomes were obtained. Physiological saline was eluted and the blank liposome ex...

Embodiment 3

[0053] Embodiment 3, preparation and characterization of liposome / SCC-31 by passive drug loading method

[0054] This example discloses the preparation and characterization of liposome / molecular targeting drug SCC-31 by passive drug loading method, which specifically includes the following steps:

[0055] The membrane material formulation of liposome / SCC-31 is HSPC / Chol / mPEG 2000 - DSPE (50:45:5, molar ratio), respectively weigh the above membrane materials and dissolve them in ethanol, and inject them dropwise into 0.9% normal saline under the condition of magnetic stirring. Ultrasonic cell pulverizer ultrasonicated for 10min (80w, ultrasonic 2s, interval 1s) to obtain liposome / SCC-31. The particle diameter of the liposome / SCC-31 measured by a Malvern laser scattering particle size analyzer was 124.27 nm, and the PDI was 0.201. The encapsulation efficiency of liposome measured by HPLC was 85.56%, the drug loading capacity was 8.91%, and the drug concentration contained in t...

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Abstract

The invention belongs to the field of biological medicines, and relates to a molecular targeting drug-entrapped liposome and application of the liposome in preparation of a drug for treating tumors. The molecular targeting drug-entrapped liposome is composed of a molecular targeting drug, and lipidosome components such as phospholipid, cholesterol, mPEG-DSPE and/or targeting molecule modified PEG-DSPE. The liposome is prepared by loading a molecular targeting drug into a water phase or phospholipid bilayer in a liposome in an active or passive drug loading manner so that tumor targeting drug delivery can be realized, and the anti-tumor effect, especially the anti-brain tumor effect, of the molecular targeting drug is remarkably enhanced. Furthermore, the combination of the molecular targeting drug-entrapped liposome and pharmaceutically acceptable medicinal components and/or diluents can be prepared into various dosage forms for targeting treatment of tumors and has potential clinicalapplication value.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a liposome carrying molecular targeting drugs and its application in preparing drugs for treating tumors. Background technique [0002] The prior art discloses that molecular targeted drugs are mainly targeted at the key targets of malignant tumor occurrence and development for therapeutic intervention. Because they can selectively kill tumor cells, they have good tolerance and low toxicity. Compared with traditional cytotoxic drugs Anticancer drugs have greater advantages. According to reports, some molecular targeted drugs have shown better efficacy in the corresponding tumor treatment. Molecular targeted drugs can be divided into single-target inhibitors and multi-target inhibitors. Currently known single-target inhibitors include BCr-Abl kinase inhibitors (such as imatinib, dasatinib, ponatinib, etc.) Ni, etc.), epidermal growth factor (EGFR) inhibitors (such as gefit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K45/00A61P35/00
CPCA61K9/127A61K9/0019A61K47/24A61K47/28A61K45/00A61P35/00
Inventor 陆伟跃王晓艺李锦阳谢操
Owner FUDAN UNIV
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