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

A technology of epirubicin and drugs, which is applied in the field of medicine, can solve problems such as impact, difficult connection and non-toxic degradation, delivery reliability of small molecule drug epirubicin, limited clinical application of epirubicin drugs, etc.

Active Publication Date: 2020-04-07
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 epirubicin is one of the difficulties in solving the current limited clinical application of epirubicin.

Method used

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  • Medicine containing epirubicin, preparation method, medicine composition and application thereof
  • Medicine containing epirubicin, preparation method, medicine composition and application thereof
  • Medicine containing epirubicin, preparation method, medicine composition and application thereof

Examples

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preparation example Construction

[0160] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned medicine containing epirubicin, 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 epirubicin is mounted on the nucleic acid nanoparticles to obtain the medicine containing the epirubicin.

[0161] When physically linked, epirubicin is usually physically intercalated between GC base pairs. And when adopting covalent linking mode to link, epirubicin will usually react with the amino group outside the G ring to form a covalent link. The medicine containing epirubicin prepared by the above method can have better targeting after the target head is modified, can stably deliver epirubicin, and has high reliability.

[0162] In a preferred embodiment, the step of mounting epirubicin by physical connection includes: mixing and stirring epi...

Embodiment 1

[0184] 1. RNA and DNA nanoparticle carriers:

[0185] (1) The base sequences of the three polynucleotides that make up the RNA nanoparticles are shown in Table 1:

[0186] Table 1:

[0187] (2) Three polynucleotide base sequences of DNA nanoparticles

[0188]

[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°...

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]

[0209] Table 3: R-2

[0210]

[0211] Table 4: R-3

[0212]

[0213] Table 5: R-4

[0214]

[0215]

[0216] Table 6: R-5

[0217]

[0218] Table 7: R-6

[0219]

[0220] Table 8: R-7

[0221]

[0222]

[0223] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0224] 2. Self-assembly experimental steps:

[0225] (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;

[0226] (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;

[0227] (3) Load the pro...

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Abstract

The application provides a medicine containing epirubicin, a preparation method, a medicine composition and application thereof. The medicine comprises nucleic acid nanoparticles and the epirubicin, and the epirubicin is mounted on nucleic acid nanoparticles. Nucleic acid nanoparticles include a nucleic acid domain, and the nucleic acid domain contains a a sequence, a b sequence and a c sequence.The a sequence contains a a1 sequence or a sequence that at least one base insertion, base deletion or base substitution occurs in a1 sequence. The b sequence contains a b1 sequence or a sequence thatat least one base insertion, base deletion or base substitution occurs in b1 sequence. The c sequence contains a c1 sequence or a sequence that at least one base insertion, base deletion or base substitution occurs in c1 sequence. After the nucleic acid domain is modified by the target head, the medicine containing epirubicin provided by the present application has better targeting, can stably delivers epirubicin, and has high reliability.

Description

technical field [0001] The 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 (CSA: 56420-45-2, molecular formula: C 27 h 29 NO 11 .HCI, molecular weight: 580.0) is an anti-tumor antibiotic, which is an isomer of doxorubicin. Its mechanism of action is to directly intercalate between DNA nucleic acid base pairs, interfere with the transcription process, prevent the formation of mRNA, and thus 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 liver cancer) cell carcinoma and metastatic carcinoma) and various solid tumors such as medullary thyroid carcinoma. [0003]...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/54A61K31/704A61P35/02A61P35/00
CPCA61K47/6929A61K47/549A61K31/704A61P35/02A61P35/00
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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