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Docetaxel-containing medicine, and preparation method, pharmaceutical composition and application thereof

A docetaxel and drug technology, applied in the field of medicine, can solve the problems of the small molecule drug docetaxel delivery reliability, the limited clinical application of the docetaxel drug, the influence, the toxicity and the self-design contradiction of the transfection activity, etc.

Active Publication Date: 2020-05-19
BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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  • Docetaxel-containing medicine, and preparation method, pharmaceutical composition and application thereof
  • Docetaxel-containing medicine, and preparation method, pharmaceutical composition and application thereof
  • Docetaxel-containing medicine, and preparation method, pharmaceutical composition and application thereof

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preparation example Construction

[0156] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned drug containing docetaxel, which includes the following steps: providing any one of the above-mentioned nucleic acid nanoparticles; by means of physical connection and / or covalent connection The docetaxel is mounted on the nucleic acid nanoparticles to obtain the docetaxel-containing drug.

[0157]When physically linked, docetaxel is usually intercalated between GC base pairs by physical intercalation. In the case of covalent linkage, docetaxel usually reacts with the amino group outside the G ring to form a covalent linkage. The docetaxel-containing drug prepared by the above method can have better targeting after the target head is modified, and can stably deliver the docetaxel with high reliability.

[0158] In a preferred embodiment, the step of mounting docetaxel through physical connection includes: mixing and stirring docetaxel, nucleic ac...

Embodiment 1

[0183] 1. RNA and DNA nanoparticle carriers:

[0184] (1) The base sequences of three polynucleotides forming RNA nanoparticles are shown in Table 1:

[0185] Table 1:

[0186]

[0187]

[0188] (2) Three polynucleotide base sequences of DNA nanoparticles

[0189] The DNA uses the same sequence as the above RNA, except that T is substituted for U. Among them, the molecular weight of chain a is 8802.66, the molecular weight of chain b is 8280.33, and the molecular weight of chain c is 9605.2.

[0190] The a, b, and c strands of the above-mentioned RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0191] 2. Self-assembly experimental steps:

[0192] (1) RNA or DNA single strands a, b, and c are simultaneously mixed and dissolved in DEPC water or TMS buffer at a molar ratio of 1:1:1;

[0193] (2) Heat the mixed solution to 80°C / 95°C (the RNA assembly temperature is 80°C, and the DNA assembly temperature is 95°C),...

Embodiment 2

[0204] 1. Seven groups of short-sequence RNA nanoparticle carriers:

[0205] (1) The base sequences of the three polynucleotides of the seven groups of RNA nanoparticles are shown in Table 2 to Table 8:

[0206] Table 2: R-1

[0207]

[0208] Table 3: R-2

[0209]

[0210]

[0211] Table 4: R-3

[0212]

[0213] Table 5: R-4

[0214]

[0215] Table 6: R-5

[0216]

[0217]

[0218] Table 7: R-6

[0219]

[0220] Table 8: R-7

[0221]

[0222] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0223] 2. Self-assembly experimental steps:

[0224] (1) RNA single strands a, b, and c are simultaneously mixed and dissolved in DEPC water or TMS buffer at a molar ratio of 1:1:1;

[0225] (2) Heat the mixed solution to 80°C, keep it for 5min and then cool down slowly to room temperature at a rate of 2°C / min;

[0226] (3) Load the product onto an...

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Abstract

The invention provides a docetaxel-containing medicine, and a preparation method, a pharmaceutical composition and application thereof. The medicine comprises nucleic acid nanoparticles and docetaxel,and the docetaxel is mounted on the nucleic acid nanoparticles; the nucleic acid nanoparticles comprise a nucleic acid domain, the nucleic acid domain comprises a sequence a, a sequence b and a sequence c. The sequence a comprises a sequence a1 or a sequence in which at least one base is inserted, deleted or replaced in the sequence a1; the sequence b comprises a sequence b1 or a sequence in which at least one base is inserted, deleted or replaced in the sequence b1; and the sequence c comprises a sequence c1 or a sequence in which at least one base is inserted, deleted or replaced in the sequence c1. After the nucleic acid domain of the docetaxel-containing medicine is modified by a target head, the docetaxel-containing medicine provided by the invention has relatively good targeting property, can stably deliver the docetaxel, and is very high in reliability.

Description

technical field [0001] The application relates to the field of medicine, in particular, to a drug containing docetaxel, its preparation method, pharmaceutical composition and application. Background technique [0002] Docetaxel (Docetaxel) has the same effect as paclitaxel (PTX). It is an M-phase cycle-specific drug that promotes the polymerization of tubules into stable microtubules and inhibits their aggregation and disintegration, thereby significantly reducing the number of tubules and destroying microtubules. grid. In vitro experiments show that it has cytotoxic effect on various mouse and human tumor cell lines, and its antitumor spectrum is wider than that of PTX. [0003] At present, in order to achieve an effective therapeutic level in the tumor site, antitumor drugs including docetaxel must use large doses of chemotherapy drugs, but large doses of systemic administration may damage healthy normal cells. Adverse reactions in tissues and organs. These adverse reac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/54A61K47/69A61K31/337A61K9/51A61K47/26A61P35/00
CPCA61K47/549A61K47/6929A61K31/337A61K9/5123A61P35/00
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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