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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