Journal
NANOMEDICINE
Volume 14, Issue 7, Pages 889-910Publisher
FUTURE MEDICINE LTD
DOI: 10.2217/nnm-2018-0289
Keywords
asenapine maleate; Caco 2 cells; in vivo imaging; nanostructured lipid carriers
Funding
- Science and Engineering Research Board (SERB), Department of Science and Technology, Government of India, New Delhi
- Worldwide Cancer Research [12-1054]
- Malaysian government agency Majlis Amanah Rakyat (MARA)
- Worldwide Cancer Research [12-1054] Funding Source: researchfish
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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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