Polymer micelle lyophilized agent encapsulating insoluble antitumor drug

Abstract

The invention belongs to the field of pharmaceutical agents, relates to a polymer micelle lyophilized agent encapsulating an insoluble antitumor drug as well as a preparation method and an application thereof. The polymer micelle lyophilized agent is prepared by carrying out molecular self-assembly on a methoxy poly(ethylene glycol) 2000-polyester block copolymer to form micelles, and then encapsulating the insoluble antitumor drug in a hydrophobic core formed by the polyester. The lyophilized agent has high encapsulation rate, high drug loading and small particle size, can significantly improve the water solubility of the insoluble drug and result in passive targeting of more antitumor drugs to concentrate in the tumor tissues, thus improving an anti-tumor treatment effect and reducing the toxic and side effects of drugs, and can be used to prepare the drugs used for the treatment of lung cancer, intestinal cancer, mammary cancer, ovarian cancer, etc. The lyophilized agent can also be quickly dissolved and dispersed to form a transparent micellar solution after water for injection, normal saline solution and the like are added, and is used for the preparation of the drugs for treating primary intestinal cell carcinoma.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a freeze-dried preparation of polymer micelles loaded with insoluble antitumor drugs, in particular to a freeze-dried preparation of polymer micelles loaded with taxane-type insoluble antitumor drugs and a preparation method thereof and uses. Background technique [0002] In recent years, the incidence of tumor has risen sharply. Because of its difficult treatment and high mortality, it has become the second leading cause of human death. At present, most of the antineoplastic drugs in clinical use are hydrophobic drugs, such as paclitaxel, docetaxel, and hydroxycamptothecin, which are taxanes; although the above drugs have been widely used clinically, there are still commercially available preparations The following problems, such as, currently commonly used paclitaxel injection (Taxol, Tesu, etc.) need to add a high concentration of surfactant polyoxyethylene castor oil...

AI Technical Summary

Problems solved by technology

At present, most of the antineoplastic drugs in clinical use are hydrophobic drugs, such as paclitaxel, docetaxel, and hydroxycamptothecin, which are taxanes; although the above drugs have been widely used clinically, there are still commercially available preparations The following problems, such as, currently commonly used paclitaxel injection (Taxol, Tesu, etc.) need to add a high concentration of surfactant polyoxyethylene castor oil (Cremophor EL) and a mixed solution of absolute ethanol to improve the solubility of paclitaxel in water , but Cremophor EL releases histamine when degraded in the body, which can lead to severe allergic reactions, and can also form tiny particles in the blood, wrapping paclitaxel molecules, thereby affecting the diffusion of drug molecules to tissues and affecting the anti-tumor effect; in addition, there are studies It was found that Cremophor EL can also dissolve vinylhexyl phthalate in PVC infusion sets, causing severe toxic reactions, thereby affecting drug safety; high concentrations of Tween are also added to the commercially available preparations of docetaxel -80 is used as a solubilizer, and a large amount of Tween is likely to cause adverse reactions such as hemolysis and allergies. In order to prevent the occurrence of the above-mentioned allergic reactions, patients need to pre-treat with anti-allergic drugs such as dexamethasone before medication. Medication brings a lot of inconvenience, but also seriously affects the efficacy and safety of drugs

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