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Oxaliplatin folic acid targeted lipidosome and application thereof

A technology for targeting liposomes and oxaliplatin, which is applied in the directions of liposome delivery, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., which can solve the problem of high process requirements and low encapsulation efficiency. , expensive raw materials and other problems, to achieve the effect of simple process, high encapsulation rate, and cheap raw materials

Active Publication Date: 2013-03-27
HANGZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patents 200310124776.6, 200710025130.0 and WO / 2007 / 099377 disclose oxaliplatin long-circulation liposomes, but they either use expensive raw materials, or have high process requirements, or have low encapsulation efficiency

Method used

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  • Oxaliplatin folic acid targeted lipidosome and application thereof
  • Oxaliplatin folic acid targeted lipidosome and application thereof
  • Oxaliplatin folic acid targeted lipidosome and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1: the synthesis of folic acid coupling polyethylene glycol monostearate

[0041] Precisely weigh 0.5 g of folic acid, 0.5 mL of triethylamine, and 15 mL of DMSO to dissolve, add 0.6 g of dicyclohexylcarbodiimide (DCC), 0.26 g of N-hydroxysuccinimide (NHS), and stir at room temperature in the dark. Overnight, by-products were removed by filtration. Then add 5g of polyethylene glycol (molecular weight: 4000) monostearate, heat to 35°C to dissolve, and react overnight at 35°C to obtain a crude product. Pour it into a dialysis bag with a molecular cut-off of 3500, place it in a 500 mL beaker filled with water, stir, dialyze for two days, and freeze-dry to obtain it.

[0042] The synthetic route map is as follows:

[0043]

[0044] After synthesis, the infrared spectrum and hydrogen nuclear magnetic resonance spectrum of folic acid-coupled polyethylene glycol monostearate were investigated to study its structure. figure 1 It is the red absorption spectrum of ...

Embodiment 2

[0045] Example 2 Oxaliplatin folic acid targeting liposome 1

[0046] Direct preparation method: Dissolve 4 g of lecithin and 667 mg of cholesterol in 60 mL of dichloromethane, add 20 mL of an aqueous solution containing 80 mg of oxaliplatin, stir for 30 min, sonicate for 20 min, and remove organic matter by rotary evaporation at 40°C. Solvent, after the gel collapses, add 50 mL of an aqueous solution containing 580 mg of folic acid-polyethylene glycol monostearate and 400 mg of F68 according to the components, continue to evaporate for 30 min, homogenize under high pressure at 400 bar for 5 min, and dilute to volume with water to 100 mL, then tangential flow ultrafiltration was used to separate free oxaliplatin, ultrafiltration was performed with a tangential flow membrane bag with a molecular cut-off of 10K, water was used as the replacement liquid, ultrafiltration was repeated three times, and finally concentrated to about 1 / 4 of the original volume, the encapsulation effic...

Embodiment 3

[0047] Embodiment 3: Oxaliplatin folic acid targeting liposome 2

[0048] Direct preparation method: Dissolve 4 g of lecithin and 667 mg of cholesterol in 60 mL of dichloromethane, add 20 mL of an aqueous solution containing 80 mg of oxaliplatin, stir for 30 min, sonicate for 20 min, and remove organic matter by rotary evaporation at 40°C. Solvent, after the gel collapses, add 580 mg of folic acid-polyethylene glycol monostearate and 50 mL of aqueous solution of F68 400 mg according to the components, continue to evaporate for 30 min, homogenize under high pressure at 400 bar for 5 min, and dilute with water to 100 mL, and then use tangential flow ultrafiltration to separate free oxaliplatin, perform ultrafiltration with a tangential flow membrane bag with a molecular cutoff of 5K, use water as the replacement liquid, repeat ultrafiltration 3 times, and finally concentrate to about original 1 / 4 of the volume, the encapsulation efficiency was measured by ultrafiltration centrif...

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PUM

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Abstract

The invention discloses an oxaliplatin folic acid targeted lipidosome and an application thereof. The raw materials of the oxaliplatin folic acid targeted lipidosome comprise oxaliplatin, phospholipids, cholesterol acid, folic acid- polyethylene glycol monostearate and poloxamer F68. The structure of the folic acid- polyethylene glycol monostearate is demonstrated as follows, wherein n is equal to 45 to 136. The oxaliplatin folic acid targeted lipidosome which is prepared by the invention can be applied to preparing medicine for treating gastrointestinal tumors. Compared with the prior art, the obtained oxaliplatin folic acid targeted lipidosome has the advantages of small grain size, high entrapment efficiency, improving pharmacokinetic behavior, good targeting and enhancing antineoplastic efficacy. In addition, the cost of raw materials is low and the process is simple.

Description

(1) Technical field [0001] The invention relates to the field of drug liposomes, in particular to an oxaliplatin folic acid targeting liposome and an application thereof. (2) Background technology [0002] Oxaliplatin is a third-generation platinum-based anticancer drug. In 2004, the FDA approved oxaliplatin for injection in combination with 5-fluorouracil and folinic acid for the first-line treatment of advanced colorectal cancer. Oxaliplatin preparations currently on the market include water injection and freeze-dried powder injection. Oxaliplatin has a significant effect on advanced colorectal cancer, and can also treat other gastrointestinal tumors such as gastric cancer. However, with the extensive clinical application of oxaliplatin, its adverse reactions have been continuously discovered and reported. Neurotoxicity, gastrointestinal reactions, and bone marrow suppression are common adverse reactions. [0003] Liposome is a drug delivery system with good biocompati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/282A61K31/194A61K47/34A61P35/00A61P1/00C08G65/48
Inventor 曾昭武肖人钟王小丽王俊洁周广林刘星言
Owner HANGZHOU NORMAL UNIVERSITY
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