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

A technology of lenalidomide and drugs, which is applied in the direction of drug combination, medical preparations containing active ingredients, drug delivery, etc., can solve the problem of limited clinical application, influence, toxicity and reliability of small molecule drug lenalidomide delivery Contradictions in the design of transfection activity itself

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

Method used

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

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preparation example Construction

[0155] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned lenalidomide-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 lenalidomide is mounted on the nucleic acid nanoparticles to obtain the lenalidomide-containing drug.

[0156] When physically linked, lenalidomide typically intercalates physically between GC base pairs. However, when covalent linkage is used for linkage, lenalidomide usually reacts with the amino group outside the G ring to form a covalent linkage. The lenalidomide-containing drug prepared by the above-mentioned method can have better targeting after the target head is modified, can deliver lenalidomide stably, and has high reliability.

[0157] In a preferred embodiment, the step of mounting lenalidomide through physical connection includes: mixing ...

Embodiment 1

[0182] 1. RNA and DNA nanoparticle carriers:

[0183] (1) The base sequences of the three polynucleotides that make up the RNA nanoparticles are shown in Table 1:

[0184] Table 1:

[0185]

[0186]

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

[0188] 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.

[0189] The a, b, and c strands of the above-mentioned RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0190] 2. Self-assembly experimental steps:

[0191] (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;

[0192] (2) Heat the mixed solution to 80°C / 95°C (the RNA assembly temperature is 80°C, and the DNA assembly temperat...

Embodiment 2

[0203] 1. Seven groups of short-sequence RNA nanoparticle carriers:

[0204] (1) The base sequences of the three polynucleotides of the seven groups of RNA nanoparticles are shown in Table 2 to Table 8:

[0205] Table 2: R-1

[0206]

[0207] Table 3: R-2

[0208]

[0209]

[0210] Table 4: R-3

[0211]

[0212] Table 5: R-4

[0213]

[0214] Table 6: R-5

[0215]

[0216]

[0217] Table 7: R-6

[0218]

[0219] Table 8: R-7

[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...

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Abstract

The invention provides a lenalidomide-containing medicine, and a preparation method, a pharmaceutical composition and an application thereof. The medicine comprises a nucleic acid nanoparticle and lenalidomide, and the lenalidomide 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 lenalidomide-containing medicine has a good targeting property, can stably deliver the lenalidomide, 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 lenalidomide, its preparation method, pharmaceutical composition and application. Background technique [0002] The lenalidomide compound is a yellow solid with the chemical name 3-(7-amino-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione, from which The anti-tumor drug lenalidomide is an anti-tumor drug developed by Celgene Biopharmaceutical Company of the United States. Its chemical structure is similar to that of thalidomide, and it has multiple functions such as anti-tumor, immune regulation and anti-angiogenesis. [0003] Currently, antineoplastic drugs including lenalidomide must be administered in large doses of chemotherapy drugs in order to achieve effective therapeutic levels at the tumor site, but systemic administration of large doses may damage healthy normal cells, in a range of tissues and organ adverse reactions. These adverse reactions includ...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/69A61K47/55A61K9/51A61K47/26A61K31/454A61P35/00A61P35/02
CPCA61K47/549A61K47/6929A61K47/55A61K9/5123A61K31/454A61P35/00A61P35/02
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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