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

A technology of mitoxantrone and drugs, applied in the field of drugs containing mitoxantrone, can solve the problems of impact, toxicity and transfection activity, self-design contradictions, difficult connection and non-toxic degradation, etc.

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

Method used

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

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preparation example Construction

[0157] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned mitoxantrone-containing drug, 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 mitoxantrone is mounted on the nucleic acid nanoparticles to obtain the mitoxantrone-containing medicine.

[0158] When physically linked, mitoxantrone usually physically intercalates between GC base pairs. In the case of covalent linkage, mitoxantrone usually undergoes a chemical reaction with the exoamino group of the G ring to form a covalent linkage. The mitoxantrone-containing drug prepared by the above method can have better targeting after the target head is modified, can deliver mitoxantrone stably, and has high reliability.

[0159] In a preferred embodiment, the step of mounting mitoxantrone by physical connection includes: mixing and stirrin...

Embodiment 1

[0182] 1. RNA and DNA nanoparticle carriers:

[0183] (1) The three polynucleotide base sequences that make up the RNA nanoparticles, see Table 1 for details:

[0184] Table 1:

[0185]

[0186] (2) Three polynucleotide base sequences of DNA nanoparticles.

[0187] 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.

[0188] The a, b, and c strands of the above-mentioned RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0189] 2. Self-assembly experimental steps:

[0190] (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;

[0191] (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

[0202] 1. Seven groups of short-sequence RNA nanoparticle carriers:

[0203] (1) Seven groups of three polynucleotide base sequences that make up RNA nanoparticles:

[0204] Table 2: R-1:

[0205]

[0206]

[0207] Table 3: R-2:

[0208]

[0209] Table 4: R-3:

[0210]

[0211] Table 5: R-4:

[0212]

[0213]

[0214] Table 6: R-5:

[0215]

[0216] Table 7: R-6:

[0217]

[0218] Table 8: R-7:

[0219]

[0220]

[0221] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0222] 2. Self-assembly experimental steps:

[0223] (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;

[0224] (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;

[0225] (3) Load the product onto an 8% (m / v) non-denat...

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Abstract

The invention provides a mitoxantrone-containing medicine, and a preparation method, a pharmaceutical composition and an application thereof. The medicine comprises a nucleic acid nanoparticle and mitoxantrone, and the mitoxantrone is loaded on the nucleic acid nanoparticle; and the nucleic acid nanoparticle comprises a nucleic acid structural domain, the nucleic acid structural domain comprises asequence 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 mitoxantrone-containing medicine has a good targeting property, can stably deliver the mitoxantrone, and has a very high reliability.

Description

technical field [0001] The present application relates to the field of medicine, in particular, to a medicine containing mitoxantrone, its preparation method, pharmaceutical composition and application. Background technique [0002] Mitoxantrone (Mitoxantrone, CSA: 65271-80-9, molecular formula: C 22 h 28 N 4 o 6 , Molecular weight: 444.481) is an anti-tumor antibiotic, the mechanism of action is similar to that of doxorubicin, because it has no amino sugar structure, does not produce free radicals, and has the effect of inhibiting lipid peroxidation, so it is less toxic to the heart. It is mainly used for the treatment of breast cancer, malignant lymphoma, gastric cancer, intestinal cancer, leukemia, bladder cancer, liver cancer, multiple myeloma, malignant mesothelioma and ovarian cancer and other cancers. [0003] Currently, antitumor antibiotics, including mitoxantrone, must be administered in large doses of chemotherapy drugs in order to achieve effective therapeuti...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/69A61K9/51A61K47/26A61K31/136A61P35/00A61P35/02
CPCA61K47/549A61K47/6929A61K9/5123A61K31/136A61P35/00A61P35/02
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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