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

Research output: Contribution to journalArticle

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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Lipids
Biological Availability
Pharmaceutical Preparations
Carbidopa
Differential Scanning Calorimetry
In Vitro Techniques
Asenapine
Ileum
Design of experiments
Rats
Differential scanning calorimetry
Permeability
Diffraction
Ultrasonics
X-Rays
X rays

All Science Journal Classification (ASJC) codes

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

Cite this

Managuli, Renuka S. ; Wang, Julie T. ; Faruqu, Farid N. ; Kushwah, Varun ; Raut, Sushil Y. ; Shreya, Ajjappla B. ; Al-Jamal, Khuloud T. ; Jain, Sanyog ; Mutalik, Srinivas. / Asenapine maleate-loaded nanostructured lipid carriers : Optimization and in vitro, ex vivo and in vivo evaluations. In: Nanomedicine. 2019 ; Vol. 14, No. 7. pp. 889-910.
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Managuli, RS, Wang, JT, Faruqu, FN, Kushwah, V, Raut, SY, Shreya, AB, Al-Jamal, KT, Jain, S & Mutalik, S 2019, 'Asenapine maleate-loaded nanostructured lipid carriers: Optimization and in vitro, ex vivo and in vivo evaluations', Nanomedicine, vol. 14, no. 7, pp. 889-910. https://doi.org/10.2217/nnm-2018-0289

Asenapine maleate-loaded nanostructured lipid carriers : Optimization and in vitro, ex vivo and in vivo evaluations. / Managuli, Renuka S.; Wang, Julie T.; Faruqu, Farid N.; Kushwah, Varun; Raut, Sushil Y.; Shreya, Ajjappla B.; Al-Jamal, Khuloud T.; Jain, Sanyog; Mutalik, Srinivas.

In: Nanomedicine, Vol. 14, No. 7, 01.04.2019, p. 889-910.

Research output: Contribution to journalArticle

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AU - Wang, Julie T.

AU - Faruqu, Farid N.

AU - Kushwah, Varun

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AU - Shreya, Ajjappla B.

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