Drug containing daunorubicin, preparation method thereof, pharmaceutical composition and application thereof

Abstract

The application provides a daunorubicin-containing medicine, its preparation method, pharmaceutical composition and application. The drug includes nucleic acid nanoparticles and daunorubicin, and the daunorubicin is mounted on the nucleic acid nanoparticles; the nucleic acid nanoparticles include a nucleic acid domain, the nucleic acid domain includes a sequence, b sequence and c sequence, and the a sequence includes a1 The sequence or a1 sequence has at least one base insertion, deletion or substitution sequence, the b sequence contains the b1 sequence or the b1 sequence has at least one base insertion, deletion or substitution, and the c sequence contains the c1 sequence or the c1 sequence has at least one base substitution. Sequences of insertions, deletions or substitutions. The daunorubicin-containing drug provided by the present application, after the nucleic acid domain is modified by the target head, can have better targeting, can deliver daunorubicin stably, and has high reliability.

Description

technical field [0001] The present application relates to the field of medicine, in particular, to a daunorubicin-containing medicine, its preparation method, pharmaceutical composition and application. Background technique [0002] Daunorubicin (Daunorubicin, CSA: 20830-81-3, molecular formula: C 27 H 29 NO 10 , molecular weight: 527.52) is mainly used for acute lymphoblastic or myeloid leukemia resistant to commonly used antineoplastic drugs, but the remission period is short, so it needs to be combined with other drugs. It is orange-red needle crystal, easily soluble in water. Its aqueous solution is quite stable, and its effect is the same as that of doxorubicin. It can inhibit the synthesis of RNA and DNA by intercalating DNA, and has a particularly obvious effect on RNA, selectively acting on purine nucleosides. [0003] Currently, antitumor antibiotics, including daunorubicin, must be administered in large doses of chemotherapeutic drugs in order to achieve effect...

AI Technical Summary

Problems solved by technology

Cationic liposomes have high transfection activity in vivo and in vitro, however, because the positive charge on the surface affects their normal distribution in vivo, at the same time, cationic lipids can cause immunogenicity and inflammatory responses in animal experiments

The development of polycationic gene carriers has been relatively mature. However, it is difficult to ensure that the targeting group is on the surface of the structure in the structural design, and there is a self-design contradiction between toxicity and transfection activity. At the same time, its connection is difficult to achieve non-toxic degradation in vivo.

[0006] Therefore, how to improve the delivery reliability of the existing small molecule drug daunorubicin is one of the difficulties in solving the current limited clinical application of daunorubicin.

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