CHARACTERIZATION AND PHARMACODYNAMIC EVALUATION OF DEVELOPED MICROEMULSION FOR NASAL DRUG DELIVERY

In the present study, we had developed Asenapine maleate (ASNM) loaded microemulsion (ME) to increase the solubility of Asenapine maleate by components of microemulsion including formulation concern, characterization, mucosal diffusion, stability and nasal ciliotoxicity of Asenapine maleate microemulsion (AME). For nasal delivery of Asenapine maleate, a challenge existing in formulation development is the solubilization of poorly water-soluble Asenapine maleate. The intrinsic solubility of Asenapine maleate is about 0.0312 mg/ml. The purpose of this study was to improve the solubility and to enhance the brain uptake of Asenapine maleate through an o/w microemulsion, with suitable intranasal delivery. The optimal microemulsion formulation consisted of Oleic acid, Tween 80: Propylene glycol (PG) (3:1) and water, with a maximum solubility of Asenapine maleate and no ciliotoxicity, was developed and characterized. AME was characterized for % Transmittance, pH, viscosity, globule size, zeta potential, drug content with in-vitro release studies and Ex-vivo diffusion studies using Standard Franz Diffusion cell. Further, the behavioural studies were assessed in rats by inducing hyperactivity. The optimized microemulsion was found to be stable and transparent with average globule size 94.40 nm, PDI 0.293 and without showing any ciliotoxicity during its histopathological evaluation on goat nasal mucosa.