Adriamycin-containing medicine and preparation method thereof
A doxorubicin and drug technology, applied in the field of doxorubicin-containing drugs and their preparation, can solve the contradiction between toxicity and transfection activity, the non-nucleic acid drug delivery effect has no valuable reports, and the connection is difficult. Toxic degradation and other issues
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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 includes the following steps: providing the above-mentioned nucleic acid nanoparticles; Mounted on the nucleic acid nanoparticles to obtain a drug containing doxorubicin.
[0148] When using physical linkage, doxorubicin usually intercalates between GC base pairs by physical intercalation. In the case of covalent linkage, doxorubicin usually reacts with the amino group outside the G ring to form a covalent linkage. The doxorubicin-containing drug prepared by the above method can have better targeting after the target head is modified, can stably deliver the doxorubicin, and has high reliability.
[0149] In a preferred embodiment, the step of mounting doxorubicin through physical connection includes: mixing and stirring doxorubicin, nucleic acid nanoparticles and the first solvent to obtain a premixed system; removin...
Embodiment 1
[0169] 1. RNA and DNA nanoparticle carriers:
[0170] (1) The three polynucleotide base sequences that make up the RNA nanoparticles, see Table 1 for details:
[0171] Table 1:
[0172]
[0173] (2) Three polynucleotide base sequences of DNA nanoparticles.
[0174] 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.
[0175] The a, b, and c strands of the above-mentioned RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.
[0176] 2. Self-assembly experimental steps:
[0177] (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;
[0178] (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
[0189] 1. Seven groups of short-sequence RNA nanoparticle carriers:
[0190] (1) Seven 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] 2. Self-assembly experimental steps:
[0210] (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;
[0211] (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;
[0212] (3) Load the product onto an 8% (m / v) non-denatur...
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