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A kind of preparation method of RGD peptide and penetrating peptide R8 co-modified ergosterol combined with cisplatin active drug-loading liposome

A technology of ergosterol lipids and ergosterol lipids, which is applied in the field of drugs for the treatment of lung cancer, can solve the problems of easy drug resistance, unstable properties, and low activity, and achieve good drug effects, good targeting, and packaging The effect of high sealing rate

Active Publication Date: 2018-09-11
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • 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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  • A kind of preparation method of RGD peptide and penetrating peptide R8 co-modified ergosterol combined with cisplatin active drug-loading liposome
  • A kind of preparation method of RGD peptide and penetrating peptide R8 co-modified ergosterol combined with cisplatin active drug-loading liposome
  • A kind of preparation method of RGD peptide and penetrating peptide R8 co-modified ergosterol combined with cisplatin active drug-loading liposome

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Embodiment

[0039] A method for preparing RGD peptide and membrane-penetrating peptide R8 co-modified ergosterol combined with cisplatin active drug-loading liposome, the steps are as follows:

[0040] (1) Preparation of ergosterol liposomes: Weigh lecithin, cholesterol, and ergosterol, add chloroform to dissolve, spin-evaporate into a thin film, dry in vacuo, and use ammonium chloride solution (concentration of 0.1-1.5mmol L -1 ) for the hydration liquid to be hydrated, ultrasonically stripped, ultrasonically treated with probes under an ice bath, filtered, and extruded under high pressure to obtain ergosterol liposomes; the raw material components of ergosterol liposomes are as follows in terms of total 100%: The ergosterol is 8-15wt%, and the balance is lecithin and cholesterol, and the molar ratio of lecithin and cholesterol is 3:1-6:1. The parameters of the ultrasonic treatment of the probe are: ultrasonic time 20min, ultrasonic 2s, pause 1s, ultrasonic power 900W, high pressure extr...

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Abstract

The invention discloses a preparation method of an RGD peptide and penetrating peptide R8 co-modified ergosterol and cis-platinum active drug-loading liposome. The method comprises the main steps of ergosterol liposome preparation, ammonium chloride gradient formation, drug loading and co-modification. The method is simple in technology and easy to carry out, and the encapsulation rate of a drug is high; ergosterol is adopted to partially replace cis-platinum to exert efficacy, an ergosterol and cis-platinum active drug-loading liposome is obtained, the effect of resisting a lung cancer is guaranteed, the toxic and side effects of the 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 preparation method of RGD peptide and membrane-penetrating peptide R8 co-modified ergosterol combined with cisplatin active drug-loading liposome. 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, nucleic acid, 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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K33/24A61K47/64A61K9/127A61P35/00A61K31/575
CPCA61K9/127A61K31/575A61K33/24A61K47/42A61K2300/00
Inventor 黄绳武黄挺吴梅佳赵丹丹
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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