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Liver targeting pharmaceutical composition and its preparation method

A composition and liver-targeting technology, which is applied in the direction of drug combinations, non-active ingredients of polymer compounds, anti-tumor drugs, etc., to achieve the effect of increasing drug accumulation and intake

Inactive Publication Date: 2011-09-21
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the role of Lf as a liver-targeting ligand has not been reported

Method used

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  • Liver targeting pharmaceutical composition and its preparation method
  • Liver targeting pharmaceutical composition and its preparation method
  • Liver targeting pharmaceutical composition and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Long-circulating liposomes Lf-PEG-liposomes modified with bovine lactoferrin loaded with Coumarin-6.

[0032]The liposome formulations are SPC: CHOL: DSPE-PEG: Distearic acid-N-[carboxypropionyl-(polyethylene glycol)-succinyl] phosphatidylethanolamine (DSPE-PEG-COOH): Coumarin -6 (40:13:11:1:0.3) (unit: mg). Accurately weigh the prescribed amount of SPC, CHOL and Coumarin-6, add appropriate amount of absolute ethanol to dissolve them completely, put them in a round bottom flask, place the flask on a rotary evaporator at 50°C and evaporate under reduced pressure, remove all organic solvents, and make The lipids formed a uniform film on the inside of the flask. Add hydroxyethylpiperazineethanesulfonic acid HEPES buffer solution (20mM HEPES, 144mM NaCl, pH 7.4), put it on a rotary evaporator for 30min and slowly rotate for hydration, then homogenize under high pressure at 1000bar, and circulate 20 times. The obtained liposomes were passed through a Sephadex LH 20 column,...

Embodiment 2

[0034] Long-circulating liposomes Lf-PEG-liposomes modified with bovine lactoferrin loaded with Coumarin-6.

[0035] The liposome formulations are SPC: CHOL: DSPE-PEG: Distearic acid-N-[aminopropionyl-(polyethylene glycol)-succinyl]phosphatidylethanolamine DSPE-PEG-NH 2 : Coumarin-6 (40:13:11:1:0.3) (unit: mg). Accurately weigh the prescribed amount of SPC, CHOL and Coumarin-6, add appropriate amount of absolute ethanol to dissolve them completely, put them in a round bottom flask, place the flask on a rotary evaporator at 50°C and evaporate under reduced pressure, remove all organic solvents, and make The lipids formed a uniform film on the inside of the flask. Add HEPES buffer solution (20mM HEPES, 144mM NaCl, pH 7.4), put it on a rotary evaporator for 30min and slowly rotate for hydration, then homogenize under high pressure at 1000bar, and cycle 20 times. The obtained liposomes were passed through a Sephadex LH 20 column, eluted with HEPES buffer as the mobile phase, and...

Embodiment 3

[0037] Long-circulating liposomes Lf-PEG-liposomes modified with lactoferrin analogs loaded with Coumarin-6.

[0038] The formulations of liposomes were SPC:CHOL:DSPE-PEG:DSPE-PEG-COOH:Coumarin-6 (40:13:11:1:0.3). Accurately weigh the prescribed amount of SPC, CHOL and Coumarin-6, add appropriate amount of absolute ethanol to dissolve them completely, put them in a round bottom flask, place the flask on a rotary evaporator at 50°C and evaporate under reduced pressure, remove all organic solvents, and make The lipids formed a uniform film on the inside of the flask. Add HEPES buffer solution (20mM HEPES and 144mM NaCl, pH 7.4), put it on a rotary evaporator and slowly rotate for hydration for 30min, then homogenize under high pressure at 1000bar, and cycle 20 times. The obtained liposomes were passed through a Sephadex LH 20 column, eluted with HEPES buffer as the mobile phase, and the liposome fraction was collected to obtain common coumarin-6 liposomes. Add DSPE-PEG and DSP...

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Abstract

The invention relates to a liver targeting pharmaceutical composition. The pharmaceutical composition for liver targeting is characterized in that protein and polyethylene glycol possessing a liver targeting function modifies an antitumor drug loading by liposome. The drug is delivered to a hepatic tissue lesions zone for increasing the drug concentration in the liver tumors position and raising the therapeutic efficacy of the liver tumors.

Description

Technical field: [0001] The invention relates to a pharmaceutical composition, in particular to a liver-targeting pharmaceutical composition capable of delivering medicine to the lesion area of ​​liver tissue so as to realize targeted administration. The present invention also relates to a preparation method of the aforementioned pharmaceutical composition. Background technique: [0002] Hepatocellular carcinoma (HCC) is a common malignant tumor, ranking third in the mortality rate of malignant tumors. At present, surgical resection is the first choice for the treatment of liver cancer, and it is often used in the treatment of early liver cancer. However, liver cancer surgery often has problems such as incomplete resection and easy spread and metastasis of cancer cells. At this time, surgical resection is no longer applicable, and only palliative treatments such as chemotherapy can be used. The treatment of chemotherapy drugs is non-selective, and while killing tumor cell...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K9/127A61P1/16A61P35/00
Inventor 徐月红韦敏燕邹奇吴传斌
Owner SUN YAT SEN UNIV
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