Oldenburg K R, Vo K T, Smith G A, Selick H E
Affymax Research Institute, Palo Alto, CA 94304, USA.
J Pharm Sci. 1995 Aug;84(8):915-21. doi: 10.1002/jps.2600840803.
In recent years there has been an increased interest in the use of oligonucleotides as therapeutic agents. Oligonucleotide therapeutics may have significant potential over traditional drugs due to their high degree of specificity and increased affinity. The major drawbacks to the use of oligonucleotide therapeutics are the problems associated with their delivery and their relative instability in serum. The serum instability problem has been partially overcome through the use of oligonucleotides with modified backbones. Transdermal electrotransport may be used to overcome the problems associated with delivery. Here we report the use of transdermal electrotransport in the delivery of oligonucleotides across hairless mouse skin. The effects of pH, salt concentration, current density, and oligonucleotide concentration, structure, and length have been investigated.
近年来，人们对使用寡核苷酸作为治疗剂的兴趣日益增加。寡核苷酸疗法可能比传统药物具有更大的潜力，因为它们具有高度的特异性和更高的亲和力。使用寡核苷酸疗法的主要缺点是与它们的递送相关的问题以及它们在血清中的相对不稳定性。通过使用具有修饰骨架的寡核苷酸，血清不稳定性问题已得到部分克服。经皮电转运可用于克服与递送相关的问题。在此，我们报告了经皮电转运在将寡核苷酸递送至无毛小鼠皮肤中的应用。研究了pH值、盐浓度、电流密度以及寡核苷酸浓度、结构和长度的影响。
