Drug containing doxorubicin and preparation method thereof
A doxorubicin and drug technology, applied in the field of doxorubicin-containing drugs and their preparation, can solve the problem of difficult connection, non-toxic degradation, self-design contradiction between toxicity and transfection activity, and non-nucleic acid drug delivery effects are of no value reports, etc.
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[0147] According to another aspect of the present invention, there is also provided a method for preparing the above-mentioned drug containing doxorubicin, which comprises the following steps: providing the above-mentioned nucleic acid nanoparticles; Mounted on nucleic acid nanoparticles to obtain a drug containing doxorubicin.
[0148] When physically linked, doxorubicin is usually physically intercalated between the GC base pairs. When the covalent connection is used for connection, doxorubicin usually chemically reacts with the amino group outside the G ring to form a covalent connection. The drug containing doxorubicin prepared by the above method has good targeting ability after modification of the target head, can deliver doxorubicin stably, and has high reliability.
[0149] In a preferred embodiment, the step of mounting doxorubicin by physical connection includes: mixing and stirring doxorubicin, nucleic acid nanoparticles and the first solvent to obtain a premixed s...
Embodiment 1
[0169] 1. RNA and DNA nanoparticle carriers:
[0170] (1) The three polynucleotide base sequences that make up the RNA nanoparticle are specifically shown in Table 1:
[0171] Table 1:
[0172]
[0173] (2) Three polynucleotide base sequences of DNA nanoparticles.
[0174] The DNA adopts the same sequence as the RNA described above, except that T replaces U. Among them, the molecular weight of the a chain is 8802.66, the molecular weight of the b chain is 8280.33, and the molecular weight of the c chain is 9605.2.
[0175] The a, b and c chains of the above RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.
[0176] Second, the self-assembly experimental steps:
[0177] (1) Dissolve RNA or DNA single strands a, b, and c in DEPC water or TMS buffer at a molar ratio of 1:1:1;
[0178] (2) Heating the mixed solution to 80°C / 95°C (wherein the RNA assembly temperature is 80°C and the DNA assembly temperature is 95°C), ...
Embodiment 2
[0189] 1. 7 groups of short-sequence RNA nanoparticle carriers:
[0190] (1) 7 groups of three polynucleotide base sequences that make up RNA nanoparticles:
[0191] Table 2: R-1:
[0192]
[0193]
[0194] Table 3: R-2:
[0195]
[0196] Table 4: R-3:
[0197]
[0198] Table 5: R-4:
[0199]
[0200]
[0201] Table 6: R-5:
[0202]
[0203] Table 7: R-6:
[0204]
[0205] Table 8: R-7:
[0206]
[0207]
[0208] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.
[0209] Second, the self-assembly experimental steps:
[0210] (1) Mix and dissolve RNA single strands a, b, and c simultaneously in DEPC water or TMS buffer at a molar ratio of 1:1:1;
[0211] (2) heating the mixed solution to 80°C, keeping the temperature for 5min and then slowly cooling to room temperature at a rate of 2°C / min;
[0212] (3) Load the product onto an 8% (m / v) ...
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