Tailoring Nanostructured Lipid Carriers for Efficient Delivery of Asenapine Maleate in Antipsychotic Treatment

Abstract

Asenapine Maleate (ASPM), is the atypical antipsychotic agent used for treating various psychological disorders such as schizophrenia and acute mania associated with bipolar disorder. However, the drug's therapeutic potential is intricately linked to its solubility, bioavailability, stability, and ability to be delivered specifically to the central nervous system. The aim of the study was to design, develop, and optimize Nanostructured Lipid Carriers (NLCs) encapsulating Asenapine maleate to improve the therapeutic efficacy. The development utilized a systematic approach; various formulation parameters such as lipid composition, surfactant concentration, and entrapment efficiency were meticulously optimized by employing quality-by-design principles. The optimized ASPM-loaded NLCs demonstrated a particle size of 97.6 ± 2.48 nm, zeta potential of −20mV, and entrapment efficiency of 96.74%, respectively. ASPM-loaded NLC showed initially rapid release (20%) accompanied by sustained release (75%) over 24 hr with 22-fold improvement in oral bioavailability with significantly reduced locomotor count induced by L-DOPA-carbidopa in comparison with the pure drug in Sprague-Dawley rats. Furthermore, in-vitro and in-vivo results underscored the enhanced permeability through the blood-brain barrier with superior pharmacokinetics for the NLC. Collectively, this research elucidates the potential of optimized NLCs as robust drug delivery system for asenapine maleate, offering a promising avenue for advancing therapeutic results in the management of psychosis.