Medicine containing oxaliplatin as well as preparation method, pharmaceutical composition and application thereof
An oxaliplatin and drug technology, which is applied in the field of oxaliplatin-containing drugs, can solve the problems of difficult connection, non-toxic degradation, limited delivery reliability of small-molecule drug oxaliplatin, and limited clinical application of oxaliplatin drugs. Problems such as the self-design contradiction between toxicity and transfection activity
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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 oxaliplatin-containing drug, which includes the following steps: providing any of the above-mentioned nucleic acid nanoparticles; and by means of physical connection and / or covalent connection The oxaliplatin is mounted on nucleic acid nanoparticles to obtain a drug containing oxaliplatin.
[0155] When physical connection is used, oxaliplatin is usually inserted between GC base pairs in a physical intercalation form. When a covalent connection is used for connection, oxaliplatin usually chemically reacts with the amino group outside the G ring to form a covalent connection. The oxaliplatin-containing medicine prepared by the above-mentioned method has good targeting ability after modification of the target head, can deliver oxaliplatin stably, and has high reliability.
[0156] In a preferred embodiment, the step of mounting oxaliplatin by means of p...
Example Embodiment
[0178] Example 1
[0179] 1. RNA and DNA nanoparticle carrier:
[0180] (1) The base sequences of the three polynucleotides that make up RNA nanoparticles are shown in Table 1:
[0181] Table 1:
[0182]
[0183] (2) Three polynucleotide base sequences of DNA nanoparticles
[0184] DNA uses the same sequence as the above RNA, 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.
[0185] The a, b, and c strands of the aforementioned RNA nanoparticles and DNA nanoparticles are all commissioned to synthesize by Sangong Bioengineering (Shanghai) Co., Ltd.
[0186] 2. Self-assembly experiment steps:
[0187] (1) Mix RNA or DNA single strands a, b, and c in DEPC water or TMS buffer at a molar ratio of 1:1:1;
[0188] (2) Heat the mixed solution to 80°C / 95°C (where the RNA assembly temperature is 80°C and the DNA assembly temperature is 95°C), hold it for 5 minutes a...
Example Embodiment
[0198] Example 2
[0199] 1. 7 groups of short-sequence RNA nanoparticle carriers:
[0200] (1) The base sequences of the three polynucleotides that make up the 7 groups of RNA nanoparticles are shown in Tables 2 to 8 respectively:
[0201] Table 2: R-1
[0202]
[0203] Table 3: R-2
[0204]
[0205] Table 4: R-3
[0206]
[0207] Table 5: R-4
[0208]
[0209] Table 6: R-5
[0210]
[0211] Table 7: R-6
[0212]
[0213] Table 8: R-7
[0214]
[0215] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers are all commissioned by Shenggong Bioengineering (Shanghai) Co., Ltd. to synthesize.
[0216] 2. Self-assembly experiment steps:
[0217] (1) Mix RNA single strands a, b, and c in DEPC water or TMS buffer at a molar ratio of 1:1:1;
[0218] (2) Heat the mixed solution to 80°C, keep it for 5 minutes, and then slowly lower the temperature to room temperature at a rate of 2°C / min;
[0219] (3) Load the product on an 8% (m / v) non-denaturing PAGE gel and purify th...
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