Self Emulsifying Drug Delivery System for Enhanced Solubility of Asenapine Maleate: Design, Characterisation, In Vitro, Ex Vivo and In Vivo Appraisal

AbstractSelf emulsifying drug delivery systems (SES) were developed to improve oral bioavailability of asenapine maleate (ASM), an antipsychotic drug with challenging amphiphobic nature and extensive pre-systemic metabolism.ASM-SES was prepared by choosing the proportion of oil, surfactant, co-surfactant from constructed phase diagram. The in vitro and ex vivo evaluation was done. In vivo evaluation was done through pharmacokinetic and pharmacodynamic studies. Role of lymphatic absorption was studied by lymphatic absorption inhibition study. Formulation consisting of 9.9%, 59.4%, 29.7% and 1% of oil, surfactant, co-surfactant and drug respectively was considered as optimized formulation. After various evaluation test, the globule size and zeta potential for optimised formulation (SES4) were found to be 137.9 nm and -28.8 mV respectively. A maximum of 99.64 ± 0.16% of ASM was released from SES4 in 60 minutes of time. The flux (ex vivo study) increased by 2.33 folds, which prove the enhanced release and per...