Di-demethoxycurcumin precursor liposome and preparation method thereof

Abstract

The invention provides a precursor liposome containing di-demethoxycurcumin and a preparation method capable of industrial application. The weight ratio of the di-demethoxycurcumin to phospholipids together with phospholipid derivatives is 1:5-65, 3 to 20 portions of cholesterol together with derivatives thereof and 0.5 to 5 portions of surfactant are prepared into a freeze-dried powder injection according to the portion ratio of the phospholipids to freeze-drying protective agents being 1:0.25-4. The invention relates to a novel technique and a device for preparing a precursor liposome by an efficient jetting-mixing method, has the advantages of good process reproducibility, controllable technical parameters and the like, and can provide a unilocular liposome with fat-soluble medicaments which are stably wrapped in a phospholipid bilayer. The liposome has the average particle size of between 80 and 300 nm, is narrow in the distribution range of particle size, has entrapment rate of more than 85 percent, is low in leakage rate, and is significantly improved in the stability of preparation storage process. The in vivo circulation time of the novel preparation is obviously prolonged during intravenous injection administration, and the AUC of the novel preparation is 2.67 times that of the common injection.

Description

technical field [0001] The invention belongs to the field of biomedicine and targeted preparations, relates to a proliposome of bisdemethoxycurcumin and a preparation method thereof, and provides a device and new technology for producing proliposomes by a high-efficiency jet mixing method Specifically, it is a preparation method for bisdemethoxycurcumin proliposome freeze-dried powder injection for intravenous injection. technical background [0002] Curcuminoids (curcuminoids) are the main active ingredients of the traditional Chinese medicine turmeric. The three monomers are curcumin (curcumin 1), demethoxycurcumin (curcumin 2) and bisdemethoxycurcumin. (bisdemethoxycurcumin, curcumin 3). Studies have shown that curcuminoids have various pharmacological activities such as anti-cancer, anti-inflammation, anti-oxidation and anti-virus, and have potential advantages in cancer treatment [Chen Minjuan et al. Research progress and application prospects of curcumin. 2003, 15 (1)...

AI Technical Summary

Problems solved by technology

[0004] Scholars at home and abroad expect to increase the in vivo absorption by improving the solubility of drugs. CN 1883497A discloses a method for preparing freeze-dried powder injection of curcumin 1 using cyclodextrin inclusion technology. The solvent method of chloroform and methanol is used for cyclodextrin inclusion , can lead to toxicity problems of organic solvent residues

CN1709228A discloses a preparation method of curcumin 1 solid dispersion. Curcumin 1 and polyvinylpyrrolidone are dissolved in propanol or isopropanol, and the solvent is removed by distillation under reduced pressure. The solubility of the drug increases to a certain extent, but there is no disclosure of solid dispersion. In Vivo Data for Dispersion Formulations

There are still physical stability problems such as oxidative degradation of some drugs in the lipid membrane during liposome storage, easy aggregation and fusion, and leakage, lower encapsulation efficiency and larger particle size of the lyophilized product after reconstitution and other phenomena

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