Subject Area

Pharmaceutical Technology


Pregabalin is a γ-aminobutyric acid analogue used for the treatment of neuropathic pain, seizures, and anxiety disorders. After oral administration, its level of brain penetration is rather modest. In this research, pregabalin was formulated successfully as a nanoemulsion. To track the biodistribution of pregabalin nanoemulsion in vivo, radiolabelling of pregabalin using 99mTc was performed. The different factors affecting radiolabeling yield were studied and radiolabelling yield of 92.6 % was achieved. A biological evaluation was performed in Swiss Albino mice through comparing biodistribution of intranasal (IN) 99mTc-pregabalin nanoemulsion with intravenous (IV) 99mTc-pregabalin solution at different time intervals. Biodistribution results show a noticeable higher brain uptake of radioactivity for IN 99mTc-pregabalin nanoemulsion compared to IV 99mTc-pregabalin solution at all time intervals. These results suggest that I.N. pregabalin nanoemulsion may be a useful strategy for enhancing pregabalin delivery to the brain.