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本文研究寡核苷酸是否可以直接通过粘膜和皮肤吸收,Benzylamine修饰的寡核苷酸用示踪物~(32)P标记,分别经小鼠鼻腔、阴道、口腔、直肠及耳轮皮肤给药,20min后处死,器官称重,测放射性强度。首次发现以上所有给药方法均使寡核苷酸迅速聚集到血液中,但经口,鼻给药者器官中标记物浓度比直肠,阴道给药者高5～10倍。经皮应用寡核苷酸水制剂,仅在肝,肾中出现小量放射活性;而应用“去污活性制剂”则使标记物在各器官中浓度明显升高;经皮合用电泳法给药也能使体内浓度进一步增高。经鼻给药时血中寡核苷酸可达3μmol/L,已是基
In this paper, whether the oligonucleotide can be absorbed directly through the mucosa and the skin was studied. The Benzylamine modified oligonucleotide was labeled with (32) P tracer and administered to the skin of mice nasal, vaginal, oral, rectal and helical respectively, After 20min sacrifice, organ weighing, measuring radioactivity intensity. It was first discovered that all of the above administration methods allow oligonucleotides to rapidly accumulate in the blood, but the concentration of the marker in organs of the oral and nasal administration is 5 to 10 times higher than those in the rectum and vagina. Transdermal application of oligonucleotide aqueous solution, only in the liver, kidney appear a small amount of radioactivity; and the application of “decontamination active agent” is markedly increased concentrations of the marker in various organs; percutaneous use of electrophoresis Can also make the body to further increase the concentration. Nasal administration of blood oligonucleotides up to 3μmol / L, has been based