Tiagabine Incorporated Polymeric Microneedles: Formulation and Characterization Studies

Abstract

Background: The oral route is the primary route for both acute and chronic treatment of epilepsy. However, lack of oral access during the seizures and high drug resistance limit the anti-epileptogenic effects of most antiepileptic drugs. Therefore, alternative routes and novel drug delivery systems are required. In this study, polymeric microneedles were formulated and characterized for possible intranasal administration of Tiagabine (TIA) in order to overcome the blood-brain barrier (BBB). Methods: In our study, carboxymethyl cellulose (CMC) and Eudragit® S 100 (ES100) based polymeric microneedles were formulated by micro-molding SEM, DSC, XRD, FT-IR, 1H-NMR, in vitro release, and texture analyses were performed. For the stability analyses, formulations were kept at 25 °C ± 2 °C (60 ± 5% Relative Humidity; RH), 40 °C ± 2 °C (75 ± 5% RH) and 5 °C ± 3 °C for six months. Results: Analysis results revealed that robust microneedles were formulated successfully by micromolding method with adjustable needle lengths. Depending on the polymer type, sustained TIA releases up to 72 hours were achieved. Structural integrities were maintained at all storage conditions during the storage period of six months. Conclusion: TIA-loaded microneedles have the potential with less invasive properties, even with small amounts of TIA, through the unconventional nasal route for effective treatment of epilepsy.