Drug containing pirarubicin, preparation method for drug, pharmaceutical composition and application of drug

A technology of pirarubicin and drugs, which is applied in the field of drugs containing pirarubicin, can solve the problem of difficult non-toxic degradation of connection, limited clinical application of small molecule drug pirarubicin delivery reliability, toxicity and transfection activity Problems such as self-design contradictions

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

Method used

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  • Drug containing pirarubicin, preparation method for drug, pharmaceutical composition and application of drug
  • Drug containing pirarubicin, preparation method for drug, pharmaceutical composition and application of drug
  • Drug containing pirarubicin, preparation method for drug, pharmaceutical composition and application of drug

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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 drug containing pirarubicin, 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 pirarubicin is mounted on the nucleic acid nanoparticles to obtain the pirarubicin-containing medicine.

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

[0162] In a preferred embodiment, the step of mounting pirarubicin by physical connection includes...

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]

[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°...

Embodiment 2

[0210] 1. Seven groups of short-sequence RNA nanoparticle carriers:

[0211] (1) The base sequences of the three polynucleotides of the seven groups of RNA nanoparticles are shown in Table 2 to Table 8:

[0212] Table 2: R-1

[0213]

[0214] Table 3: R-2

[0215]

[0216] Table 4: R-3

[0217]

[0218] Table 5: R-4

[0219]

[0220] Table 6: R-5

[0221]

[0222] Table 7: R-6

[0223]

[0224] Table 8: R-7

[0225]

[0226] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0227] 2. Self-assembly experimental steps:

[0228] (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;

[0229] (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;

[0230] (3) Load the product onto an 8% (m / v) non-denaturing...

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Abstract

The application provides a drug containing pirarubicin, a preparation method for the drug, a pharmaceutical composition and application of the drug. The drug comprises a nucleic acid nanoparticle andthe pirarubicin, and the pirarubicin is deposited on the nucleic acid nanoparticle; the nucleic acid nanoparticle includes a nucleic acid domain; the nucleic acid domain includes an a sequence, a b sequence and a c sequence; the a sequence includes an a1 sequence or a sequence of insertion, deletion or substitution of at least one base of the a1 sequence; the b sequence includes a b1 sequence or asequence of insertion, deletion or substitution of at least one base of the b1 sequence; and the c sequence includes a c1 sequence or a sequence of insertion, deletion or substitution of at least onebase of the c1 sequence. After the nucleic acid domain is modified by a target head, the drug containing the pirarubicin has a relatively good targeting property, can stably deliver the pirarubicin,and has very high reliability.

Description

technical field [0001] The application relates to the field of medicine, in particular, to a medicine containing pirarubicin, its preparation method, pharmaceutical composition and application. Background technique [0002] Pirarubicin (Pirarubicin, CSA: 72496-41-4, molecular formula: C 32 h 37 NO 12 , Molecular weight: 627.636) is an anti-tumor antibiotic, the mechanism of action is directly intercalated between DNA double strands, inhibits DNA polymerase, prevents nucleic acid synthesis, prevents cells from dividing in G2 phase, and leads to tumor cell death. It is mainly used to treat breast cancer, and it also has certain curative effects on malignant tumors such as head and neck cancer, bladder cancer, ureter cancer, renal pelvis cancer, ovarian cancer and cervical cancer. [0003] Currently, antitumor antibiotics, including pirarubicin, must be administered in large doses of chemotherapy drugs in order to achieve effective therapeutic levels at the tumor site, but s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K47/54A61K47/69A61P35/00
CPCA61K47/6929A61K47/549A61K31/7048A61P35/00
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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