Title:Tiagabine Incorporated Polymeric Microneedles: Formulation and
Characterization Studies
Volume: 6
Issue: 1
Author(s): Kadir Aykaç and Ebru Başaran*
Affiliation:
- Department of Pharmaceutical Technology, Faculty of Pharmacy, Anadolu University, 26470 Tepebaşı, Eskişehir, Türkiye
Keywords:
Tiagabine, epilepsy, microneedle, polymeric drug delivery systems, micromolding method, texture analysis, 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 antiepileptogenic
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 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 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.
