Cytarabine-containing medicine, and preparation method, pharmaceutical composition and an application thereof
A cytarabine and drug technology, applied in the field of preparation of cytarabine-containing drugs, can solve the problems of difficult connection, non-toxic degradation, influence, toxicity and self-design contradiction of transfection activity, etc.
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[0154] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned cytarabine-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 cytarabine is mounted on the nucleic acid nanoparticles to obtain the cytarabine-containing drug.
[0155] When physically linked, cytarabine is usually intercalated between GC base pairs by physical intercalation. In the case of covalent linkage, cytarabine usually undergoes a chemical reaction with the amino group outside the G ring to form a covalent linkage. The drug containing cytarabine prepared by the above method can have better targeting after the target head is modified, and can stably deliver cytarabine with high reliability.
[0156] In a preferred embodiment, the step of mounting cytarabine by means of physical connection includes: mixing an...
Embodiment 1
[0180] 1. RNA and DNA nanoparticle carriers:
[0181] (1) The base sequences of the three polynucleotides that make up the RNA nanoparticles are shown in Table 1:
[0182] Table 1:
[0183]
[0184] (2) Three polynucleotide base sequences of DNA nanoparticles
[0185] 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.
[0186] The a, b, and c strands of the above-mentioned RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.
[0187] 2. Self-assembly experimental steps:
[0188] (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;
[0189] (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
[0200] 1. Seven groups of short-sequence RNA nanoparticle carriers:
[0201] (1) The base sequences of the three polynucleotides of the seven groups of RNA nanoparticles are shown in Table 2 to Table 8:
[0202] Table 2: R-1
[0203]
[0204]
[0205] Table 3: R-2
[0206]
[0207] Table 4: R-3
[0208]
[0209] Table 5: R-4
[0210]
[0211]
[0212] Table 6: R-5
[0213]
[0214] Table 7: R-6
[0215]
[0216] Table 8: R-7
[0217]
[0218] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.
[0219] 2. Self-assembly experimental steps:
[0220] (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;
[0221] (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;
[0222] (3) Load the product onto an...
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