Managuli, Renuka S and Raut, Sushil Y and Ajjappla, Shreya B and Mutalik, Srinivas (2019) Asenapine maleate-loaded nanostructured lipid carriers: optimization and in vitro, ex vivo and in vivo evaluations. Nanomedicine, 14 (7). pp. 889-910. ISSN 1743-5889

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Abstract

To prepare nanostructured lipid carriers (NLCs) loaded with asenapine maleate (ASPM) to increase its oral bioavailability by intestinal lymphatic uptake. Materials & methods: ASPM-NLCs were prepared by ultrasound dispersion technique, by adopting Design of Experiment approach, and characterized. Results:The optimized formulation exhibited good physicochemical parameters. Differential scanning calorimetry and x-ray diffraction studies indicated the amorphized nature of ASPM in lipid matrix. In vitro drug release study indicated the sustained release of drug from NLCs. ASPM-NLCs showed greater permeability across Caco2 cells and everted rat ileum. ASPM-NLCs showed greater cellular uptake, superior preclinical oral bioavailability and higher efficacy in reducing the L- OPA-carbidopa-induced locomotor count compared with plain drug. Conclusion: ASPM-NLCs were successfully developed that showed enhanced performance both in vitro and in vivo/

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