Asenapine maleate-loaded nanostructured lipid carriers: Optimization and in vitro, ex vivo and in vivo evaluations

Renuka S. Managuli, Julie T. Wang, Farid N. Faruqu, Varun Kushwah, Sushil Y. Raut, Ajjappla B. Shreya, Khuloud T. Al-Jamal, Sanyog Jain, Srinivas Mutalik

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Abstract

Aim: 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-DOPA-carbidopa-induced locomotor count compared with plain drug. Conclusion: ASPM-NLCs were successfully developed that showed enhanced performance both in vitro and in vivo.

Original languageEnglish
Pages (from-to)889-910
Number of pages22
JournalNanomedicine
Volume14
Issue number7
DOIs
Publication statusPublished - 01-04-2019

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All Science Journal Classification (ASJC) codes

  • Bioengineering
  • Medicine (miscellaneous)
  • Biomedical Engineering
  • Materials Science(all)

Cite this

Managuli, R. S., Wang, J. T., Faruqu, F. N., Kushwah, V., Raut, S. Y., Shreya, A. B., Al-Jamal, K. T., Jain, S., & Mutalik, S. (2019). Asenapine maleate-loaded nanostructured lipid carriers: Optimization and in vitro, ex vivo and in vivo evaluations. Nanomedicine, 14(7), 889-910. https://doi.org/10.2217/nnm-2018-0289