Quinine drug-vincristine drug co-carried liposome and preparation method thereof

Abstract

The invention discloses a quinine drug-vincristine drug co-carried liposome and a preparation method thereof. The liposome comprises drugs, a phospholipid, a cholesterol compound and an aqueous medium, wherein the mass ratio of the drugs, the phospholipid and the cholesterol compound is 1:(2-100):(1-35), and the drugs comprise a quinine drug and a vincristine drug. With utilization of the synergistic effect of the quinine drug and the vincristine drug, the quinine drug-vincristine drug co-carried liposome has the characteristics of inhibition of multidrug resistance and reduction of medicating toxicity. The preparation method of the co-carried liposome is simple in preparation process, mild in conditions, fewer control parameters, beneficial for reducing the production cost, and easy to industrially produce.

Description

technical field [0001] The invention relates to the technical field of liposome medicines, in particular to a liposome co-loaded with quinine medicines and vincristine medicines and a preparation method thereof. Background technique [0002] Tumor is one of the main diseases that threaten human health, and chemotherapy drugs have always occupied an irreplaceable position in the treatment of tumors. However, due to the extensive use of chemotherapy drugs, tumor cells are prone to multidrug resistance (MDR) to chemotherapy drugs, and the generation of MDR is one of the main reasons for the failure of current tumor chemotherapy. [0003] Vincristine (Vincristine, VCR) is a dimeric indole-type alkaloid extracted from the flowers and leaves of Apocynaceae Changchun. Since it came out in 1962, it has been widely used as an anti-tumor drug. VCR has significant anti-tumor activity against acute lymphoblastic leukemia, breast cancer, bronchial lung cancer, Hodgkin's and non-Hodgkin...

AI Technical Summary

Problems solved by technology

At present, vincristine preparations that have been approved for clinical use or are undergoing clinical evaluation are mainly liposome preparations, such as vincristine liposome for injection, trade name Marqibo, although the therapeutic dose of the drug is reduced to a certain extent, and the The neurotoxicity of vincristine and its toxicity to normal cells, but there are still problems that it is easy to make cells resistant to the drug and the anticancer effect is not good.

In addition, existing vincristine liposomes for injection, such as Chinese invention patent ZL200410014200.9, Chinese invention patent application CN201210030558.5, etc., which can be used for intravenous injection of vincristine sulfate liposomes, all have the potential to make cells The problem of poor anticancer effect caused by drug resistance

[0007] Chinese invention patent application CN02820117.5 discloses a promicelle composition, which has a composition containing a center of a pharmaceutically active ingredient, wherein the center is encapsulated in an esterified C 12 -C 18 In the film of fatty acid, and the concentration of said fatty acid in the composition is lower than 15wt.%, its center can contain a hydrophilic phase containing vincristine or quinine and a surface active phase containing cholesterol, phospholipids, lipophilic Liposomes with a continuous hydrophilic phase of agents and unesterified fatty acids; the invention mainly utilizes the center to encapsulate 12 -C 18 Membrane promicelle composition of fatty acids in the mammalian intestine, exposed to C 12 -C 18 Fatty acids will lead to the conversion of promicelles into stable micelles, so as to effectively transport the active ingredients of drugs into the circulatory system. The research does not involve research on the interaction between multiple drugs, reducing the multidrug resistance of anticancer drugs, etc.

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