Formulation and Evaluation of Asenapine Maleate Loaded Niosomes for the Treatment of Schizophrenia

Abstract:

Background: Niosomes are the non-ionic surface-active agent primarily based vesicles. The Key obstacle of Asenapine maleate have oral bioavailability (<2%) and extensive first pass effect. Objectives: The objective key of the existing work was to formulate Asenapine maleate loaded niosomes using quality by design and rectify it with some evaluation parameters to increase bioavailability, to lead better therapeutic effect and to minimize the side effects. Methods: Formulation of niosomes was done by three methods organic solvent injection method. Factorial design (3²) experiments are significantly used to screen and to observe the effect of independent variables cholesterol and span 60 (X₁, X₂) on dependent variables particle size and entrapment efficiency (Y₁, Y₂). Results: The results revealed optimized formulation ASP-niosome A2 amongst other formulations which was found lowest particle size 84 ± 5 nm and highest % EE 70 ± 2.0%. In-vitro drug release of optimized noisome was found 68 ± 1.20 % at the end of 8 hr and zeta potential was -17.53mV which stabilized the niosomal suspension. Characterization by SEM not only indicated the spherical shape of the niosomes but also confirmed the formation of vesicle. Locomotor activity was found to be significant in in-vivo pharmacodynamic study. Pharmacokinetic study carried out and it showed C_max and t_1/2 of 16.12ng/mL and 37.18 hr which is better than reported parameters for drug. Conclusion: Thus, concluded that Asenapine maleate loaded niosomes having effective anti-psychotic activity with increased bioavailability could be prepared successfully by organic solvent injection method using span 60 and cholesterol.

Key words: IJPER, Citation profile, Scientometrics, Pharmaceutics, Journal evaluation.