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Vincristine nano targeting slow-release long-circulation liposome and preparation method thereof

A long-circulation liposome and vincristine technology, applied in the field of medicine, can solve the problems of easy fusion and aggregation during storage and application, difficulty in multi-functional modification, poor physical and chemical stability, etc., to achieve adjustable sustained release time, The effect of short preparation cycle and strong drug loading capacity

Inactive Publication Date: 2011-10-26
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Liposomes are currently one of the common means of preparations to reduce drug toxicity, but conventional liposomes prepared from traditional lecithin and cholesterol are mostly swallowed by the reticuloendothelial system (RES) in the body and reside in the blood circulation. Stay for a short time
Moreover, its physical and chemical stability is poor, fusion and aggregation are prone to occur during storage and application, and the encapsulated drug is easy to leak; there are few functional groups, and it is difficult to perform multifunctional modification, etc.

Method used

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  • Vincristine nano targeting slow-release long-circulation liposome and preparation method thereof
  • Vincristine nano targeting slow-release long-circulation liposome and preparation method thereof
  • Vincristine nano targeting slow-release long-circulation liposome and preparation method thereof

Examples

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Embodiment 1

[0031] PEG-OQLCS preparation process. Weigh 0.3g of OQLCS and dissolve in 10mL of distilled water for use; weigh 0.2g of monocarboxylated polyethylene glycol and dissolve in 10mL of distilled water, weigh 1g of EDC and add it to the aqueous solution of monocarboxylated polyethylene glycol, then weigh NHS 0.6g was added to monocarboxylated polyethylene glycol aqueous solution, and after 10 minutes, the above solution was added to OQLCS aqueous solution, and reacted for 12 hours. After the reaction, dialyzed with 8000-14000 dialysis bag for 1 day, and freeze-dried to obtain PEG- OQLCS.

[0032] FA-OQLCS preparation process. Folic acid was dissolved in 60 mL of DMSO, 1 mL of triethylamine was added thereto, 1 g of EDC and 0.6 g of NHS were dissolved with a small amount of DMSO, and then added to the above reaction system for 12 h in the dark. The product was filtered to obtain NHS-FA active lipid as a yellow solid. Dissolve NHS-FA active lipid in 50mL DMSO, and add 0.3g OQLCS....

Embodiment 2

[0034]PEG-OQLCS preparation process. Weigh 0.4g of OQLCS and dissolve in 10mL of distilled water for use; weigh 0.6g of monocarboxylated polyethylene glycol and dissolve in 10mL of distilled water, weigh 2g of EDC and add it to the aqueous solution of monocarboxylated polyethylene glycol, then weigh NHS 1.3g was added to monocarboxylated polyethylene glycol aqueous solution, and after 25 minutes, the above solution was added to OQLCS aqueous solution, and reacted for 18 hours. After the reaction, dialyzed with 8000-14000 dialysis bag for 4 days, and freeze-dried to obtain PEG- OQLCS.

[0035] FA-OQLCS preparation process. Dissolve folic acid in 80 mL of DMSO, add 3 mL of triethylamine to it, dissolve 2 g of EDC and 1.3 g of NHS with a small amount of DMSO, and then add them to the above reaction system to avoid light for more than 18 h. The product was filtered to obtain NHS-FA active lipid as a yellow solid. Dissolve NHS-FA active lipid in 65mL DMSO, and add 0.4g OQLCS. u...

Embodiment 3

[0037] PEG-OQLCS preparation process. Weigh 0.5g of OQLCS and dissolve it in 10mL distilled water for use; weigh 1.0g of monocarboxylated polyethylene glycol and dissolve it in 10mL of distilled water, weigh 3g of EDC and add it to the aqueous solution of monocarboxylated polyethylene glycol, then weigh NHS 2.0g was added to the monocarboxylated polyethylene glycol aqueous solution, and after 40 minutes, the above solution was added to the OQLCS aqueous solution, and reacted for 24 hours. After the reaction, dialyzed with 8000-14000 dialysis bag for 7 days, and freeze-dried to obtain PEG- OQLCS.

[0038] FA-OQLCS preparation process. Dissolve folic acid in 100mL of DMSO, add 5mL of triethylamine to it, dissolve 3g of EDC and 2.0g of NHS with a small amount of DMSO, and add them to the above reaction system to avoid light for more than 24h. The product was filtered to obtain NHS-FA active lipid as a yellow solid. Dissolve NHS-FA active lipid in 80mL DMSO, and add 0.5g OQLCS....

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Abstract

The invention relates to a vincristine nano targeting slow-release long-circulation liposome and a preparation method thereof. The uniform particle size of the liposome is in the range of 50-200 nm, and polyethylene glycol and folic acid are rich on the surfaces of the liposome particles. The ratio in parts by mass of raw materials is that folate-conjugated octadecyl-quaternized lysine modified chitosan (FA-OQLCS): PEGlated octadecyl-quaternized lysine modified chitosan (PEG-OQLCS): vincristine=1: (1-2): (0.5-1); the ratio of the total amount of FA-OQLCS and PEG-OQLCS to cholesterol=(4-2):1; the liposome is prepared by a reverse-phase evaporation method or thin-film dispersion method; the entire preparation method is simple and rapid, the preparation period is short, and the drug loading rate of the prepared polymer liposome is up to 9.7%; and the surface polyethylene glycol modification enables the polymer liposome not to be easily caught by a human reticulo-endothelial system and prolongs the circulation time of the polymer liposome, and the folate modification contributes to the tumor targeting property of the polymer liposome.

Description

technical field [0001] The invention relates to a vincristine nano-targeted sustained-release long-circulation liposome and a preparation method thereof, belonging to the technical field of medicines. Background technique [0002] Vincristine is an active ingredient extracted from the vinca flower of the Apocynaceae plant. The target of anti-tumor effect is microtubules, which mainly inhibits the polymerization of tubulin and affects the formation of spindle microtubules, so that mitosis stops in metaphase. It can also interfere with protein metabolism and inhibit the activity of RNA polymerase, and inhibit the synthesis of cell membrane lipids and the transport of amino acids on the cell membrane. Vincristine has effects on acute leukemia, acute lymphoblastic leukemia, malignant lymphoma, germ cell tumor, small cell lung cancer, Ewing sarcoma, Wilms tumor, neuroblastoma, breast cancer, chronic lymphocytic leukemia, gastrointestinal cancer, melanin tumor and multiple myelo...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/475A61K47/36A61P35/00
Inventor 常津王生苏文雅王汉杰康世胤
Owner TIANJIN UNIV
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