Medicine containing docetaxel, its preparation method, pharmaceutical composition and application

Abstract

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

Description

technical field [0001] The present application relates to the field of medicine, in particular, to a docetaxel-containing medicine, its preparation method, pharmaceutical composition and application. Background technique [0002] Docetaxel has the same effect as paclitaxel (PTX) and is a specific drug for the M phase cycle, promoting the polymerization of small tubules into stable microtubules and inhibiting their polymerization, thereby significantly reducing the number of small tubules and destroying microtubules grid. In vitro experiments show that it has cytotoxic effect on a variety of mouse and human tumor cell lines, and its anti-tumor spectrum is wider than that of PTX. [0003] At present, in order to achieve an effective therapeutic level at the tumor site, anti-tumor anti-drugs including docetaxel must apply large doses of chemotherapy drugs, but systemic administration of large doses may damage healthy normal cells, resulting in a series of Causes adverse react...

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 docetaxel is one of the difficulties in solving the current limited clinical application of docetaxel

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