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In vivo study of structural integrity determination of antisense to NF-kB oligonucleotides in rat serum

机译:测定大鼠血清中NF-kB寡核苷酸反义序列的结构完整性的体内研究

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Antisense is a promising drug which is considered as next generation drug due to its high specific nature to its target. Nonetheless it has a number of drawbacks, which, in fact, can be overcome by microencapsulating the drug with biodegradable and biocompatible polymer. However, characterization and quantisation of the encapsulated antisense is critical for determination of administered doses and for pharmacokinetic study. Specially, the drug integrity after administration is important to determine. Also for clinical use, the drug is radiated with gamma radiation, which might cause changes in the drug or polymer of the microsphere depending on the radiation intensity. Therefore, it is also required to determine the structural integrity of the irradiated microsphere. Previously we have demonstrated the integer form of gamma radiated and non-radiated microsphere in vitro (1). Here we have determined the structural integrity of the radiated and nonOradiated microsphere in vivo by HPLC.
机译:反义是一种很有前途的药物,由于其对靶标的高度特异性,因此被认为是下一代药物。然而,它具有许多缺点,实际上,可以通过用可生物降解和生物相容的聚合物将药物微囊化来克服。但是,封装反义物的表征和定量对于确定给药剂量和药代动力学研究至关重要。特别地,给药后的药物完整性是确定的重要因素。同样对于临床使用,用γ射线辐射药物,根据辐射强度,这可能引起药物或微球聚合物的变化。因此,还需要确定被辐照的微球的结构完整性。以前,我们已经证明了体外γ辐射和非辐射微球的整数形式(1)。在这里,我们已经通过HPLC确定了体内辐射和非辐射微球的结构完整性。

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