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RGD peptide and penetrating peptide R8 co-modified ergosterol and cis-platinum active drug-loading liposome

A technology of ergosterol lipids and ergosterol, which is applied in the field of drugs for the treatment of lung cancer, can solve the problems of low activity, unstable properties, and easy drug resistance, etc., achieve good targeting, reduce toxic and side effects, and have good drug effects Effect

Active Publication Date: 2016-07-27
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, gastrointestinal toxicity, ototoxicity, and neurotoxicity cannot be ignored; (2) have low activity against certain cancer cells, such as breast cancer, colon cancer, etc.; (3) are prone to drug resistance; (4) only Slightly soluble in water, unstable in nature, decomposed when exposed to light, its aqueous solution will undergo hydrolysis and become invalid after being placed at room temperature, and will be transformed into transplatinum, which is toxic but has no tumor inhibitory effect

Method used

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  • RGD peptide and penetrating peptide R8 co-modified ergosterol and cis-platinum active drug-loading liposome
  • RGD peptide and penetrating peptide R8 co-modified ergosterol and cis-platinum active drug-loading liposome
  • RGD peptide and penetrating peptide R8 co-modified ergosterol and cis-platinum active drug-loading liposome

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Embodiment

[0039] A RGD peptide and membrane-penetrating peptide R8 co-modify ergosterol combined with cisplatin active drug-loading liposome, which consists of ergosterol combined with cisplatin active drug-loaded liposome, RGD cyclic peptide (DSPE-PEG3400-c, commercially available) and Penetrating peptide R8 (DSPE-PEG1000-R8, commercially available) was prepared by incubating in a water bath at 55°C for 1 hour; the ergosterol combined with cisplatin active drug-loaded liposomes was composed of ergosterol liposomes and cisplatin solution Made from raw materials, wherein the mass ratio of ergosterol to cisplatin is controlled to be 1:1-4:1; the ergosterol liposome is made of ergosterol 8-15wt% and liposome 85-92%, The liposome is composed of lecithin and cholesterol, and the molar ratio of lecithin and cholesterol is 3:1-6:1; the amount of RGD cyclic peptide and penetrating peptide R8 is controlled as RGD cyclic peptide: penetrating peptide R8: cholesterol The molar ratio is 0.07:0.07:1....

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Abstract

The invention discloses an RGD peptide and penetrating peptide R8 co-modified ergosterol and cis-platinum active drug-loading liposome which is prepared through incubation of an ergosterol and cis-platinum active drug-loading liposome, RGD cyclic peptide and penetrating peptide R8 in a water bath. The ergosterol and cis-platinum active drug-loading liposome is prepared from an ergosterol liposome and a cis-platinum solution, the ergosterol liposome is prepared from 8 wt%-15 wt% of ergosterol and 85%-92% of liposomes, and the liposomes are composed of lecithin and cholesterol. According to the RGD peptide and penetrating peptide R8 co-modified ergosterol and cis-platinum active drug-loading liposome, ergosterol is adopted to partially replace cis-platinum to exert efficacy, the effect of resisting a lung cancer is guaranteed, the toxic and side effects of a drug are significantly reduced, and damage to human bodies is small; meanwhile, the RGD peptide and the penetrating peptide R8 serve as target heads, the targeting property is good, and the drug exertion effect is good.

Description

technical field [0001] The invention relates to a medicine for treating lung cancer, in particular to a liposome actively loaded with ergosterol combined with cisplatin co-modified by RGD peptide and membrane-penetrating peptide R8. Background technique [0002] Antrodia Antrodia mainly contains polysaccharides, triterpenoids, proteins, vitamins, trace elements and other chemical components, in addition, there are superoxide dismutase (SOD), adenosine, accounting, lectin, amino acids, sterols, lignin , blood pressure stabilizing substances, etc. Triterpenoids are considered to be one of the only sources of the bitterness of Antrodia camphorata, present in mycelium and fruiting bodies. So far, nearly 30 kinds of triterpenoids have been discovered, mainly two parent structures of lanosterane and ergosterane. [0003] Antrodia cintrodia was first consumed by humans to relieve hangovers and treat liver diseases. In recent years, it has also been extensively studied, further co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/24A61K47/42A61K9/127A61P35/00A61K31/575A61K33/243
CPCA61K9/127A61K31/575A61K47/42A61K33/243A61K33/24A61K2300/00A61K9/1278A61P35/00
Inventor 黄绳武黄挺吴梅佳赵丹丹
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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