Medicine containing epirubicin, preparation method thereof, pharmaceutical composition and application thereof

Abstract

The present application provides a medicine containing epirubicin, its preparation method, pharmaceutical composition and application. The drug includes nucleic acid nanoparticles and epirubicin, and epirubicin 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 epirubicin-containing medicine provided by the present application can have good targeting ability after the nucleic acid domain is modified by the target head, can deliver epirubicin stably, and has high reliability.

Description

technical field [0001] The present application relates to the field of medicine, in particular, to a medicine containing epirubicin, its preparation method, pharmaceutical composition and application. Background technique [0002] Epirubicin (Epirubicin, CSA: 56420-45-2, molecular formula: C 27 H 29 NO 11 .HCI, molecular weight: 580.0) is an anti-tumor antibiotic and an isomer of doxorubicin. Its mechanism of action is to directly intervene between DNA nucleic acid base pairs, interfere with the transcription process, prevent the formation of mRNA, and thereby inhibit DNA , RNA and protein synthesis. It is a cell cycle non-specific drug that is effective against a variety of transplanted tumors, including acute leukemia and malignant lymphoma, breast cancer, bronchial lung cancer, ovarian cancer, Wilms tumor, soft tissue sarcoma, liver cancer (including primary hepatic cell carcinoma and metastatic carcinoma) and a variety of solid tumors such as medullary thyroid carcin...

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 epirubicin is one of the difficulties in solving the current limited clinical application of epirubicin.

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