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

A paclitaxel and drug technology, applied in the field of medicine, can solve problems such as the contradiction between toxicity and transfection activity, the difficulty of non-toxic degradation of the connection, and the difficulty of ensuring the targeting group.

Active Publication Date: 2020-04-24
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 paclitaxel is one of the difficulties in solving the current limited clinical application of paclitaxel.

Method used

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  • Paclitaxel-containing medicine, and preparation method, pharmaceutical composition and application thereof
  • Paclitaxel-containing medicine, and preparation method, pharmaceutical composition and application thereof
  • Paclitaxel-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 paclitaxel-containing drug, which includes the following steps: providing any one of the above-mentioned nucleic acid nanoparticles; Loaded on nucleic acid nanoparticles to obtain paclitaxel-containing drugs.

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

[0158] In a preferred embodiment, the step of mounting paclitaxel through physical connection includes: mixing and stirring paclitaxel, nucleic acid nanoparticles and the first solvent to obtain a premi...

Embodiment 1

[0183] 1. RNA and DNA nanoparticle carriers:

[0184] (1) The base sequences of the three polynucleotides that make up the 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 tempera...

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 paclitaxel-containing medicine, and a preparation method, a pharmaceutical composition and an application thereof. The medicine comprises a nucleic acid nanoparticle and paclitaxel, and the paclitaxel is loaded on the nucleic acid nanoparticle; and the nucleic acid nanoparticle comprises a nucleic acid structural domain, the nucleic acid structural domain comprises a sequence a, a sequence b and a sequence c, the sequence a comprises a sequence a1 or a sequence obtained by inserting, deleting or substituting at least one base in the sequence a1, the sequence b comprises a sequence b1 or a sequence obtained by inserting, deleting or substituting at least one base in the sequence b1, and the sequence c comprises a sequence c1 or a sequence obtained by inserting, deleting or substituting at least one base in the sequence c1. After the nucleic acid structural domain is modified with a target head, the paclitaxel-containing medicine has a good targeting property, can stably deliver the paclitaxel, and has a very high reliability.

Description

technical field [0001] The present application relates to the field of medicine, in particular, to a drug containing paclitaxel, its preparation method, pharmaceutical composition and application. Background technique [0002] Paclitaxel, also known as paclitaxel, taxol, porphyrin, and special element, is the best natural anticancer drug that has been discovered so far. It has been widely used in the treatment of breast cancer, ovarian cancer, some head and neck cancers and lung cancer in clinical practice. As a diterpene alkaloid compound with anticancer activity, paclitaxel has attracted botanists and chemists due to its novel and complex chemical structure, extensive and significant biological activities, new and unique mechanism of action, and scarce natural resources. The great favor of scientists, pharmacologists, and molecular biologists made it a world-renowned anti-cancer star and research focus in the second half of the 20th century. [0003] Currently, antineopla...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K47/54A61K47/69A61K9/51A61K47/26A61P35/00
CPCA61K31/337A61K47/549A61K47/6929A61K9/5123A61P35/00
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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