Irinotecan hydrochloride and doxorubicin hydrochloride co-loaded liposome and preparation method thereof

A technology of irinotecan hydrochloride and doxorubicin hydrochloride, which is applied in the field of irinotecan hydrochloride and doxorubicin hydrochloride co-loaded liposomes and its preparation, can solve the problems of toxicity and further research, and achieve delayed release, Improved drug delivery efficiency and high loading capacity

Active Publication Date: 2019-03-29
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

(Ishaque M.Shaikh, Kuan-Boone Tan, Anumita Chaudhury, Yuanjie Liu, Bee-Jen Tan, Bernice M.J.Tan, Gigi N.C.Chiu. Liposome co-encapsulation of synergistic combination of irinotecan and doxorubicin for the treatment of intraperitoneally grown ovarian tumor. xenogra Journal of Controlled Release 172 2013:852–861.) However, the problem with this method lies in the continuous accumulation of heavy metal ions in the body, which may cause toxicity, and the safety of ionophore A23187 needs further study

Method used

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  • Irinotecan hydrochloride and doxorubicin hydrochloride co-loaded liposome and preparation method thereof
  • Irinotecan hydrochloride and doxorubicin hydrochloride co-loaded liposome and preparation method thereof
  • Irinotecan hydrochloride and doxorubicin hydrochloride co-loaded liposome and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0047] Embodiment 1: film dispersion method

[0048] Combine DSPC, Cholesterol and MPEG 2000 -DSPE was mixed at a weight ratio of 3:1:0.05, dissolved in absolute ethanol, evaporated under reduced pressure to form a film, added 0.6M TEA-SOS solution, and hydrated at 65°C for 1 hour to obtain heterogeneous multilocular liposomes. Use high-pressure extrusion equipment to reduce the particle size of liposomes, then use Sephadex G-50 to remove anions from the outer phase of blank liposomes by column chromatography, and replace it with a solution containing 20mM HEPES and 150mM NaCl to form a transmembrane kinetic gradient. According to irinotecan: doxorubicin: phospholipid (weight ratio) is 0.4:0.4:1, first add irinotecan solution to blank liposomes, incubate at 65°C for 30min, then add doxorubicin solution and incubate for 30min, namely Co-loaded liposomes with irinotecan and doxorubicin.

Embodiment 2

[0049] Embodiment 2: ethanol injection method

[0050] Combine DSPC, Cholesterol and MPEG 2000 - DSPE is mixed in a weight ratio of 3:1:0.05, dissolved in absolute ethanol, stirred in a water bath at 65°C, evaporated to remove ethanol under reduced pressure, then added 0.6M TEA-SOS solution, hydrated at 65°C for 1 hour, and obtained inhomogeneous multilamellar liposomes. Use a high-pressure extrusion device to reduce the particle size of the liposomes, then use Sephadex G-50 to remove the anions of the outer phase of the blank liposome, and replace it with a solution containing 20mM HEPES and 150mM NaCl. According to irinotecan: doxorubicin: phospholipid (weight ratio) is 0.4:0.4:1, first add irinotecan solution to blank liposomes, incubate at 65°C for 30min, then add doxorubicin solution and incubate for 30min, namely Co-loaded liposomes with irinotecan and doxorubicin.

Embodiment 3

[0052] Combine DSPC, Cholesterol and MPEG 2000 - DSPE was mixed in a weight ratio of 3:1:0.1, dissolved in absolute ethanol, evaporated under reduced pressure to form a film, added 0.6M TEA-SOS solution, and hydrated at 65°C for 1 hour. The particle size was reduced using high-pressure extrusion equipment, and then Sephadex G-50 was used to remove anions from the outer phase of the liposome and replace it with a solution containing 20 mM HEPES and 150 mM NaCl. According to irinotecan: doxorubicin: phospholipid (weight ratio) is 0.4:0.4:1, load irinotecan solution first, then load doxorubicin solution, and incubate at 65°C to obtain irinotecan and doxorubicin co-loaded fat plastid.

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Abstract

The invention belongs to the technical field of medicines, and relates to an irinotecan hydrochloride and doxorubicin hydrochloride co-loaded liposome and a preparation method thereof. The liposome comprises the following components of medicines, phosphatide, cholesterol, triethylammonium sucrose octasulfate salt and a buffering agent, wherein the medicines include irinotecan hydrochloride and doxorubicin hydrochloride, the weight ratio of the irinotecan hydrochloride to the doxorubicin hydrochloride is (1-10) to (1-10), the weight ratio of the irinotecan hydrochloride to the phosphatide is (0.1-1) to 1, and the weight ratio of the phosphatide to the cholesterol is (2-9) to 1. The liposome is high in encapsulation efficiency and high in medicine loading quantity and can co-deliver two kinds of medicines, the situation that the medicines can maintain cooperating proportion when reaching tumor positions is guaranteed, and the purposes of improving effects and reducing toxin can be achieved.

Description

Technical field: [0001] The invention relates to the technical field of liposome medicaments, in particular to a liposome co-loaded with irinotecan hydrochloride and doxorubicin hydrochloride and a preparation method thereof. Background technique: [0002] The pathogenesis of malignant tumors is complicated and there are many treatment links. For this heterogeneous polygenic disease, a single therapeutic agent often cannot achieve the desired therapeutic effect. Combination therapy has become the standard treatment in the clinical practice of most malignant tumors. [0003] Irinotecan (irinotecan, IRI, CPT-11), a camptothecin-like prodrug, acts on topoisomerase I by converting topoisomerase I into a topoisomerase I-drug-DNA complex substances, thereby inhibiting DNA replication and exerting anti-tumor effects. Irinotecan can be used to treat colorectal cancer, small cell lung cancer, non-small cell lung cancer, cervical cancer, ovarian cancer, breast cancer, malignant lymp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/26A61K47/28A61K31/4745A61K31/704A61P35/00
CPCA61K9/127A61K31/4745A61K31/704A61K47/26A61K47/28A61P35/00A61K2300/00
Inventor 王永军刘洁如杨文倩王振杰叶智鹏何仲贵
Owner SHENYANG PHARMA UNIVERSITY
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