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Taxol nano targeting slow-release long-circulating liposome and preparation method thereof

A long-circulating liposome and paclitaxel technology, applied in the field of medicine, can solve the problems of drug systemic toxicity, short residence time, cumbersome use process, etc., and achieve the effects of uniform and controllable particle size, good preparation stability and simple preparation process.

Inactive Publication Date: 2010-07-21
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0004] 2. The preparation process is too cumbersome and inconvenient
Due to the possible allergic reactions of paclitaxel preparations containing polyoxyethyl castor oil, before using such preparations, antiallergic drugs must be taken or injected, making the use process cumbersome
Moreover, if this type of preparation is diluted during clinical use and placed for 24 hours, granular precipitates will be precipitated, which must be filtered to remove the granular precipitates, otherwise it will bring great danger to the clinic
[0005] 3. Paclitaxel has low utilization efficiency, high toxicity and high cost of use
Due to the lack of targeting of this type of paclitaxel preparations, it is easy to cause the systemic distribution of the drug to cause systemic toxicity, and the drug concentration in the tumor tissue is lower than the killing concentration
Clinically, the goal of killing tumor cells can only be achieved by increasing the dosage of the drug, which not only increases the cost of treatment for the patient, but also increases the pain caused by the toxicity of paclitaxel.
[0006] 4. Traditional preparations have a short circulation time in the body
Traditional paclitaxel preparations are easily captured by phagocytes of the reticuloendothelial system (RES) after entering the human body, and are removed from the blood circulation system, thereby reducing the amount of drug reaching the tumor tissue site
[0007] 5. Traditional preparations do not have sustained-release function and cannot maintain effective drug concentration for a long time
Traditional paclitaxel preparations do not have the protection and barrier of drug carriers, directly enter the blood circulation system through intravenous injection, are quickly cleared by the reticuloendothelial system (RES), and stay in the blood for a short time, which is not conducive to the absorption of tumor tissues and pathological sites

Method used

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  • Taxol nano targeting slow-release long-circulating liposome and preparation method thereof
  • Taxol nano targeting slow-release long-circulating liposome and preparation method thereof
  • Taxol nano targeting slow-release long-circulating liposome and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0045] Folate receptor mediates synthesis of polyethylene glycol-modified chitosan derivatives. Weigh 0.3 g of the prepared amphiphilic carboxymethyl chitosan stearyl ammonium chloride and dissolve in 10 mL of water; weigh 0.6 g of monocarboxylated polyethylene glycol and dissolve in 10 mL of water; mix the two evenly and add Coupling agent ethyl-(3-dimethylpropyl)carbodiimide hydrochloride (EDC) 1.4g, stirring reaction at room temperature for 24h; Dry to obtain ethylene glycol-modified chitosan derivatives. Dissolve 0.6g of folic acid in 50ml of dimethylsulfoxide solution, add 1.5ml of triethylamine to it, mix 1.5g of coupling agent N-hydroxysulfosuccinimide (NHS) with a certain amount of dimethylsulfoxide After the sulfone is dissolved, it is added to the above reaction system and reacted in the dark for more than 12 hours. The product was filtered to obtain activated folic acid as a yellow solid. The activated folic acid was dissolved in 25ml dimethyl sulfoxide, and 0.3g...

Embodiment 2

[0047] Folate receptor mediates synthesis of polyethylene glycol-modified chitosan derivatives. Weigh 0.4 g of the prepared amphiphilic carboxymethyl chitosan stearyl ammonium chloride and dissolve in 10 mL of water; weigh 0.2-0.6 g of monocarboxylated polyethylene glycol and dissolve in 10 mL of water; mix the two evenly Then add coupling agent ethyl-(3-dimethylpropyl)carbodiimide hydrochloride (EDC) 1g, stir and react at room temperature for 24h; Freeze-dry to obtain ethylene glycol-modified chitosan derivatives. Dissolve 0.2 g of folic acid in 50 ml of dimethyl sulfoxide solution, add 1.5 ml of triethylamine to it, mix 1 g of coupling agent N-hydroxysulfosuccinimide (NHS) with a certain amount of dimethyl sulfoxide After dissolving, add it to the above reaction system and react in the dark for more than 12 hours. The product was filtered to obtain activated folic acid as a yellow solid. The activated folic acid was dissolved in 25ml dimethyl sulfoxide, and 0.4g of ethyle...

Embodiment 3

[0049] Folate receptor mediates synthesis of polyethylene glycol-modified chitosan derivatives. Weigh 0.5 g of the prepared amphiphilic carboxymethyl chitosan stearyl ammonium chloride and dissolve in 10 mL of water; weigh 0.2-0.6 g of monocarboxylated polyethylene glycol and dissolve in 10 mL of water; mix the two evenly Then add coupling agent ethyl-(3-dimethylpropyl)carbodiimide hydrochloride (EDC) 1.5g, stir and react at room temperature for 24h; , lyophilized to obtain ethylene glycol-modified chitosan derivatives. Dissolve 0.4g of folic acid in 50ml of dimethylsulfoxide solution, add 1.5ml of triethylamine to it, mix 1.4g of coupling agent N-hydroxysulfosuccinimide (NHS) with a certain amount of dimethylsulfoxide After the sulfone is dissolved, it is added to the above reaction system and reacted in the dark for more than 12 hours. The product was filtered to obtain activated folic acid as a yellow solid. The activated folic acid was dissolved in 25ml dimethyl sulfoxi...

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Abstract

The invention relates to a taxol nano targeting slow-release long-circulating liposome and a preparation method thereof. The taxol nano targeting slow-release long-circulating liposome of the invention mediates the structure of polyethylene glycol modificatory chitosan derivative by folate receptor; and the invention utilizes the chitosan derivative as an auxiliary material to prepare a novel taxol preparation by a reverse phase evaporation method or film dispersion method, and the prepared taxol nano targeting slow-release long-circulating liposome has the grain size smaller than 100nm, can freely run in the blood, penetrates the endothelial cell of a target tissue, can be uptaken by a tumor cell to enter the cell, releases the contained taxol in the cell, and greatly improves the utilization efficiency of medicaments. In addition, the surface of the prepared taxol nano targeting slow-release long-circulating liposome is also covered by a layer of polyethylene glycol (PEG) which can prolong the dwell time of liposome in the blood, reduce the uptaken amount of liposome by liver and spleen reticuloendothelial systems, and is beneficial to the absorption of tumor tissues and lesion parts.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a paclitaxel nano-targeted sustained-release long-circulation liposome and a preparation method thereof. Background technique [0002] Paclitaxel (PTX) is an anticancer drug extracted from Taxus genus plants, and has certain curative effects on advanced ovarian cancer, breast cancer, and lung cancer. However, its water solubility is extremely poor. In order to increase its solubility, the paclitaxel preparations commercialized at home and abroad all adopt the same formula, that is, a solubilizer polyoxyethyl castor oil (Cremophorel) is added to the paclitaxel ethanol injection. But this type of paclitaxel preparation itself has insurmountable defects, and the main defects are as follows: [0003] 1. The solubilizer polyoxyethyl castor oil can produce side effects such as allergies and cause pain to patients. The polyoxyethyl castor oil in the preparation will cause the release...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61K47/36A61K47/34A61K47/22A61P35/00A61K47/10
Inventor 王汉杰苏文雅康世胤胡秀凤常津
Owner TIANJIN UNIV
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