Polyethylene glycol-distearoyl phosphatidyl ethanolamine derivant and preparation method thereof
A derivative and amide-forming technology, applied in the field of derivatives of novel polyethylene glycol-distearoyl phosphatidyl ethanolamine, can solve the problems of limited tumor cell affinity and the like
Active Publication Date: 2010-10-20
北京中海康医药科技发展有限公司
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Although liposomes containing RGD ligands have the effect of targeting tumors, most of them are monovalent ligands with limited affinity with tumor cells
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The invention discloses a polyethylene glycol (PEG)- distearoyl phosphatidyl ethanolamine (DSPE) derivant shown in a formula (I) and a preparation method thereof (n in the formula is an integral number from 0 to 9). The RDG modified DSPE-PEG derivant can increase tumour affinity to meet the requirement of treatment.
Description
technical field The invention relates to a novel polyethylene glycol-distearoylphosphatidylethanolamine derivative and a preparation method thereof. Background technique Polyethylene glycol-distearoylphosphatidylethanolamine (hereinafter referred to as PEG-DSPE) is a new type of liposome carrier auxiliary material, and the liposome prepared by using this auxiliary material has the property of long circulation. A preparation using this substance as an auxiliary material has been marketed in the United States in 1995, with a trade name of DOXIL. The application of polyethylene glycol-distearoylphosphatidylethanolamine in the field of medicine has been reported in many documents, such as: [1]Influence of preparation path on the formation of discs and threadlike micelles inDSPE-PEG2000 / lipid systems.Biophysical Chemistry , 2008, 132, 97; [2] Effects of phospholipidhydrolysis on the aggregate structure in DPPC / DSPE-PEG2000 liposome preparations after gel toliquid crystalline pha...
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IPC IPC(8): C08G65/48A61K47/34
Inventor 徐庆春宋华先黄海
Owner 北京中海康医药科技发展有限公司
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