Patent number 8765181 is assigned to
The following quote was obtained by the news editors from the background information supplied by the inventors: "Vinca alkaloids antitumor agent is a class of effective broad-spectrum antitumor agent, which is important and widely used in the clinic treatment of various cancers, such as leukaemia, lymphoma, breast cancer, lung cancer, liver cancer and many other solid tumors. This class of antitumor agents mainly includes vinblastine (VLB), vincristine (VCR), vindesine (VDS) and vinorelbine (VNR). Similar to other cytotoxic antineoplastics, these antitumor agents, however, lack selectivity for tumor tissues and lead to a severe dose-dependent acute toxicity, which is represented clinically as nausea, emesis, alopecia, and blood vessel irritation. More severe are the inhibition of bone marrow and strong neurotoxicity, and repeated administration will lead to severe complications. The toxic side effect of vinca alkaloids antitumor agent greatly limits their clinic application in the long-term treatment for tumors.
"One approach to significantly decrease toxicity of vinca alkaloids antitumor agent is to alter their tissue distribution and improve their selectivity for tumor tissues. The liposome preparation of vinca alkaloids antitumor agent could reduce the toxic side effect of the agent and increase their distribution in tumor tissues, so as to mitigate their dose-dependent acute toxicity. The liposome preparation has been approved for the clinic treatment of various types of cancer and a satisfying therapeutical effect has been achieved. Two liposomal products, amphotericin liposome and paclitaxel liposome, have been approved by
"In water, amphiphilic molecules will aggregate spontaneously to form micelle when the concentration of the molecules is beyond critical micelle concentration. Taking advantage of this property, medicament is encapsulated in the hydrophobic core of the micelle. Micellar preparations have been used in clinic treatment practice for a long time. For example, deoxycholate sodium was utilized to solubilize amphotericin B and the like. A paper titled with 'polymer micelle: a novel drug carrier' by Kun etc., summarized the use of micelle as a drug carrier (Adv. Drug. Del. Rev., 21:107-116, 1976). Recently, as a targeting, long-circulating and sustained release drug carrier, polymer micelle has been paid a great attention and becomes a research focus in the drug delivery systems.
"Polyethylene glycol (PEG) is a water-soluble polymer that is stable under physiological condition. Because the space structure of PEG is capable of preventing the approach of plasma proteins, PEG has been widely used to modify the properties of phospholipid and protein drugs. In nanoparticle delivery system, PEG is capable of forming a hydrophilic protection layer on the surface of particles to prevent the aggregation of the particles, avoiding being recognized and phagocytized by reticuloendothelial system in body, and extending the retention time of drugs in blood circulation, whereby a long circulation is achieved.
In addition to the background information obtained for this patent, NewsRx journalists also obtained the inventors' summary information for this patent: "One objective of the present invention is to provide a nano-micellar preparation containing vinca alkaloids antitumor agent for intravenous injection, which is a dynamically stable system, has good stability and can be used in targeted therapy in vivo. Thus, the nano-micellar preparation is capable of improving the drug distribution in tumor tissues, increasing effectiveness and decreasing toxicity.
"Another objective of the present invention is to provide a method that producing the nano-micellar preparation containing vinca alkaloids antitumor agent for intravenous injection.
"The present invention provides a nano-micellar preparation containing vinca alkaloids antitumor agent for intravenous injection, comprising a therapeutically effective amount of vinca alkaloids antitumor agent, a phosphatide derivatized with polyethylene glycol, together with pharmaceutically acceptable adjuvants.
"In one embodiment, a nano-micellar preparation containing vinca alkaloids antitumor agent is provided, which is produced by a suitable preparation method from basic adjuvant, a phosphatide derivatized with PEG."
URL and more information on this patent, see: Liang, Wei; Lou, Min'an; Si, Wei. Nano Anticancer Micelles of Vinca Alkaloids Entrapped in Polyethylene Glycolylated Phospholipids. U.S. Patent Number 8765181, filed
Keywords for this news article include: Alkenes, Polyenes, Liposomes, Hydrocarbons, Organic Chemicals, Polyethylene Glycols,
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