Formulation and Characterization of Lacosamide-loaded Polymeric Microneedles

Abstract

Background and objectives: Epilepsy is a neural disorder that occurs because of a disruption in neural conduc-tions in various parts of the brain and is mainly characterized by seizures, pensive gaze, involuntary mimics, contractions, meaningless speeches, repetitive movements, and loss of consciousness. The serious side effects of conventional drug delivery systems due to high applied doses, low transition rates to the brain, and limitations of drug application during seizures result in the urgent need for novel drug delivery systems for the enhanced treatment of epilepsy. Methods: In this study, Lacosamide was selected because of its high therapeutic dose, which is due to its low transition to the target site. Microneedle patches were formulated by micromolding of polymers of carboxy-methyl cellulose (CMC) and Eudragit S 100 (ES100) for a unique route for applications to reduce the applied dose to minimize the severe side effects. This strategy enhanced brain transition via the nasal route and over-came the blood-brain barrier (BBB) to minimize the applied dose. Characterization studies were performed in detail. Results: The results revealed that the releases of Lacosamide extended to 96 h with ES100 microneedle patches. In contrast, CMC microneedles released almost all the active ingredients within 1 h due to the hydrophilic nature of the polymer. Stability studies indicated that the formulations were stable at 25 ± 2°C (60 ± 5% Relative Humid-ity; RH), 40 ± 2°C (75 ± 5% RH) and 5 ± 3°C for 6 months. Conclusions: By considering the film like structures, polymeric microneedle patches have the potential for Lacosa-mide delivery through the unconventional nasal route for the improved treatment of epilepsy.