Nano micelle preparation of Catharanthus roseus alkaloids antineoplastic drugs with coating of phospholipid derived from polyethylene glycol

Abstract

The invention provides intravenous nanomicelle agents of vinca alkaloids antitumor drug, it contains an effective dose for treating of vinca alkaloids antitumor drug (vinblastine and vincristine or vindesine), macrogol derivatization phospholipid, and the pharmaceutical acceptable adjuvants. Its preparation is to pack the drug in the formative nanomicelle agents, prepare and make the intravenous nanomicelle agents of vinca alkaloids antitumor drug. Vinca alkaloids antitumor drug and macrogol derivatization phospholipid form into a very uniform size nanomicelle. In micelles, polyethylene glycol molecule and hydrophobic core for drug packing form a hydrophilicitious inhibitory coating, avoid the drugs contact with the protein such as enzymes in the blood and identified and phagocytized by the endothelial system in vivo, phagocytosis, the cycle time of micellar in vivo is extended. In addition, the micellar drug also increases the storage stability and the effect on the tumor of the drug and reduces drug toxicity.

Description

technical field [0001] The invention relates to a nano-micelle preparation of an intravenously injectable vinca alkaloid antitumor drug and a preparation method thereof. Background technique [0002] Vinca alkaloid antineoplastic drugs are a class of effective and broad-spectrum important antineoplastic drugs, which are widely used clinically to treat various cancers, such as leukemia, lymphoma, breast cancer, lung cancer, liver cancer and many other solid tumors. Such antineoplastic drugs mainly include: Vinbastine (VLB), Vincristine (VCR), and Vindesine (VDS). However, like other cytotoxic antineoplastic drugs, it lacks selectivity to tumor tissue and has serious dose-dependent acute toxicity, which is clinically manifested as nausea, vomiting, hair loss, and vascular irritation. What's more serious: myelosuppression and neurotoxicity are strong, and repeated medication can lead to serious complications. The toxic and side effects of vinca alkaloid antitumor drugs seriou...

AI Technical Summary

Problems solved by technology

But vinca alkaloid antineoplastic drug liposome also has many shortcomings.

For example, the drug is encapsulated in the inner water phase, and the drug is quickly released from the liposome, resulting in instability of the preparation; the minimum particle size of the liposome is 50nm, and the liposome enters the cell often through fusion and endocytosis The mechanism is completed, usually the drug is encapsulated by liposomes, and the cytotoxic effect is weaker than that of free drugs; the preparation process of liposomes is complicated, requiring the compounding of various lipid components (at least two lipid components), particle size control Requires special equipment and devices; easy to flocculate during storage, etc.

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