Tiagabine Incorporated Polymeric Microneedles: Formulation and Characterization Studies

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Aykaç K., Başaran E.

Current Applied Polymer Science , vol.1, no.1, pp.1-12, 2023 (SCI-Expanded)


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 deliv-
ery 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 bar-
rier (BBB).
Methods: In our study, carboxymethyl cellulose (CMC) and Eudragit ® S 100 (ES100) based poly-
meric microneedles were formulated by micromolding method. Scanning electron microscopy
(SEM), differential scanning calorimetry (DSC), X-ray diffractometry (XRD), fourier transform
infrared spectroscopy (FT-IR) and proton nuclear magnetic resonance ( 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 mi-
cromolding 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 condi-
tions 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.