Novel platinum liposome preparation and preparation method thereof

A liposome and platinum-based technology, which is applied in the field of a new type of platinum-based liposome preparation method and its preparation, can solve the problems of low encapsulation rate, inactivation, and not very ideal, and achieves strong anticancer activity and stability. Good, high drug loading effect

Active Publication Date: 2014-02-12
ZHEJIANG JIANFENG HANSHENG BIOSCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the currently developed liposomes for platinum-based drugs are not very ideal, mainly due to low encapsulation efficiency, drug leakage, and inactivation of some cisplatin encapsulated in liposomes [Meric, Rixe, Khayat. Metastatic malignant melanoma. Drugs Today (Barc), 2003, 39 (S-C): 17.]

Method used

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  • Novel platinum liposome preparation and preparation method thereof
  • Novel platinum liposome preparation and preparation method thereof
  • Novel platinum liposome preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0062] 1) Weigh 5.56g of silver nitrate, dissolve it in 30ml of distilled water, put it in a 50ml Erlenmeyer flask, put it in a 60°C water bath, add 2.5g of cisplatin while stirring, and continue stirring until the reaction is complete. The method to judge whether the reaction is complete is: take a small amount of reaction solution and centrifuge, add a small amount of silver nitrate, if the solution does not become cloudy, it means that the reaction is complete, otherwise, it means that the chloride ion has not reacted completely, and the reaction should be continued until no precipitation occurs. Centrifuge the fully reacted reaction solution at 4000 rpm for 5 minutes, wash the precipitate, combine the supernatant and dilute to 50ml;

[0063] 2) Weigh 2.34g of oleic acid and dissolve it in 50ml of methanol, drop it dropwise into the above-mentioned platinum-containing solution while stirring, and react overnight in the dark, centrifuge the reaction solution at 2000rpm for 10...

Embodiment 2

[0066] 1) Weigh 5.16g of silver sulfate, dissolve it in 30ml of distilled water, place it in a 50ml Erlenmeyer flask, put it in a 60°C water bath, add 2.5g of cisplatin while stirring, and continue stirring until the reaction is complete. The method to judge whether the reaction is complete is: take a small amount of reaction solution and centrifuge, add a small amount of silver nitrate, if the solution does not become cloudy, it means that the reaction is complete, otherwise, it means that the chloride ion has not reacted completely, and the reaction should be continued until no precipitation occurs. Centrifuge the fully reacted reaction solution at 4000 rpm for 5 minutes, wash the precipitate, combine the supernatant and dilute to 50ml;

[0067] 2) Weigh 5.07g of sodium oleate into the above solution, react at room temperature for 30 minutes, add 50ml of acetone for extraction, add anhydrous magnesium sulfate to the acetone extract to remove water, filter, evaporate the filtr...

Embodiment 3

[0070] Dimyristoylphosphatidylcholine (DMPC) 475mg, dimyristoylphosphatidylglycerol (DMPG) 200mg, 50mg of the new platinum compound synthesized above, dissolved in 10ml chloroform, placed on a rotary evaporator at 35°C to recover the organic solvent under reduced pressure , forming a layer of film on the wall of the bottle, and further placed in a decompression desiccator to completely remove the organic solvent. Add distilled water for hydration for 30min, freeze-thaw repeatedly 3 times, place the liposome solution in a centrifuge at 5000 rpm for 5 minutes, and dissolve the precipitate in 20ml10% (g / ml) sucrose to obtain the platinum-based liposome solution. Further freeze-drying can obtain the freeze-dried powder of platinum liposome.

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Abstract

The invention relates to a novel platinum compound, a liposome preparation containing the compound, a preparation method of the liposome preparation and an application of the liposome preparation in tumor treatment. The main components of the platinum liposome provided by the invention include active platinum compounds, phospholipid, cholesterol, fatty acid and the like, the platinum liposome can be prepared into a freeze-dried powder injection by freeze drying, and the platinum liposome is small in particle size, high in medicine loading capacity and good in stability. The platinum liposome can improve the bioavailability of cisplatin liposome, prolong the residence time of the medicine in vivo and concentrate the cisplatin in cancerous organs, thereby not only reducing the medicine dosage and reinforcing the curative effect, but also capable of reducing the toxic side effects of the medicine, so that the platinum liposome is suitable for treating a variety of tumor diseases.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a method for preparing novel platinum-based liposomes and preparations thereof. Background technique [0002] Cisplatin (DDP) is a complex of heavy metal platinum. There are 2 chlorine atoms and 2 ammonia molecules around the central platinum atom. It has the properties of a bifunctional alkylating agent. Its chemical structure is as follows: [0003] [0004] In the human body, chlorine can be hydrolyzed to form active positively charged hydration molecules, which then react with nucleic acids and proteins, causing DNA inter-strand or intra-strand cross-links, or forming DNA-protein cross-links, thereby inhibiting DNA replication And transcription, leading to DNA breakage and error codes, inhibiting cell mitosis, and the effect is strong and long-lasting. Cisplatin has a wide anti-cancer spectrum and is a non-specific drug for the cell cycle. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00C07F19/00C07J9/00A61K9/127A61K31/282A61K31/685A61K31/575A61P35/00
Inventor 周小菊赵孝斌罗伯特·李
Owner ZHEJIANG JIANFENG HANSHENG BIOSCI
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