Page 54 - I. Chemical biology and drug discovery

[I. Chemical biology and drug discovery-30]

Pharmacokinetics and biodistribution study of miRNA-497

using capillary electrophoresis with laser induced

fluorescence detector

Haejin Kwon¹, Eunmi Ban¹, Eun Joo Song¹

¹College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 03760,

Korea

MicroRNAs (miRNAs) are involved in the pathogenesis of many human diseases, and have been widely investigated
as therapeutic agents to treat various diseases. Therefore effective and reliable analytical methods of miRNAs are

required for evaluating the pharmacokinetics (PK) and biodistribution (BD) of miRNAs as therapeutic candidates.
The capillary electrophoresis with laser-induced fluorescence (CE-LIF) method has been recently reported as a

promising and relatively rapidly developing tool with the potential to provide highly sensitive and specific analysis
of biological molecules including miRNAs. Here, the CE-LIF method was used for application in the PK and BD

studies of miRNA-497 as a model miRNA for a lung target; miRNA-497 hybridized with 6-FAM-labeled DNA probes
were separated and detected using CE-LIF. Using CE-LIF, the miRNA-497 level was evaluated in rat plasma and

organs after IV administering 1 mg/ml of a miRNA-497 mimic. Hence, miRNA-497 displayed a relatively short half-
life of 1.76 h and was delivered to the lungs but mainly accumulated in the liver and spleen. This study evaluated

the PK and BD of the miRNA-497 mimic using CE-LIF for the first time and suggested the need for further studies
to extend the half-life and conduct lung-targeted delivery of miRNA-497.