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

doi:10.2217/nnm-2018-0289

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^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

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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 language	English
Pages (from-to)	889-910
Number of pages	22
Journal	Nanomedicine
Volume	14
Issue number	7
DOIs	https://doi.org/10.2217/nnm-2018-0289
Publication status	Published - 1 Apr 2019

Keywords

asenapine maleate
Caco 2 cells
in vivo imaging
nanostructured lipid carriers

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Nanomedicine 2019 Main document Managuli RSLicence: CC BY-NC-ND

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

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.",

keywords = "asenapine maleate, Caco 2 cells, in vivo imaging, nanostructured lipid carriers",

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

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AU - Wang, Julie T.

AU - Faruqu, Farid N.

AU - Kushwah, Varun

AU - Raut, Sushil Y.

AU - Shreya, Ajjappla B.

AU - Al-Jamal, Khuloud T.

AU - Jain, Sanyog

AU - Mutalik, Srinivas

PY - 2019/4/1

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N2 - 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.

AB - 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.

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KW - Caco 2 cells

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

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Keywords

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