Abstract
Objective: To formulate and characterize Lorazepam loaded buccal patches using mucoadhesive, biodegradable, natural polymers-pectin (hydrophilic) and collagen (lipophilic) for treating epileptic seizures.
 Methods: Lorazepam loaded buccal patches were prepared by solvent casting method and were subjected to various Physico-chemical evaluation parameters to find the optimized buccal patch. The in vitro drug release study and ex vivo permeation study was carried out. The stability study and histopathological study of optimized Lorazepam loaded buccal patch was also carried out.
 Results: From in vitro drug release study, it was found that Lorazepam loaded buccal patch (B4) exhibited maximum drug release of 96.16 %±0.07 than other formulations at the end of 4 h, indicating an initial burst release followed by sustained release with release kinetics as Higuchi diffusion model. Based on the in vitro drug release, % drug content, % swelling index, folding endurance, B4 formulation was considered as optimised formulation and was further characterized. Ex vivo permeation study revealed that the cumulative amount of drug permeated from optimised Lorazepam loaded buccal patch (B4) was higher (3831.4±0.21µg/cm2) than marketed Midazolam buccal solution (1724±0.12 µg/cm2) and control drug solution (895.42±0.07 µg/cm2) with an enhancement ratio of 4.8. B4 formulation also showed a higher flux value (12.52±0.02µg/cm2/hr) compared to marketed formulation (5.732±0.01 µg/cm2) and control drug solution (2.563±0.03 µg/cm2) of P<0.05. The histopathological study using bovine buccal mucosa revealed that the B4 formulation is safe for buccal application. The stability study confirmed that B4 formulation is stable in both room and refrigeration conditions. Hence the formulated Lorazepam loaded buccal patch seems to be a promising carrier for the enhanced buccal delivery of Lorazepam in treating epileptic seizures.
 Conclusion: The formulated Lorazepam loaded collagen/pectin buccal patch was found to be an efficient and stable route for the buccal delivery of Lorazepam in treating acute epileptic seizures which could be further explored scientifically.
Highlights
Epilepsy is a disorder of the central nervous system, precisely the brain, characterized by enduring predisposition and neuronal misfiring that results in epileptic seizures [1]
Lorazepam is soluble in methanol, propanol and phosphate buffer saline (PBS pH 6.8) and is slightly soluble in distilled water and acetone
In Fourier Transform Infra-Red (FTIR) spectra of lorazepam a strong peak at 3549 cm-1 shows the presence of the hydroxy group
Summary
Epilepsy is a disorder of the central nervous system, precisely the brain, characterized by enduring predisposition and neuronal misfiring that results in epileptic seizures [1]. It causes the periodic loss of consciousness with abnormal electrical activity which either leads to convulsions or not leads to convulsions [2]. Used medications for these epileptic seizures include oral dosage forms and intravenous dosage forms These were found to be effective for management of chronic the epileptic seizures but were not effective to treat acute and immediate seizures [5,6]. The aim of our study was to develop a drug delivery system made of natural polymers only and that incorporates a rapid-acting antiepileptic drug to resolve all these disadvantages and limitations of both the drug delivery system and the drug, effective for the management of acute seizures [12,13,14,15]
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