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

Managuli, Renuka S and Raut, Sushil Y and Ajjappla, Shreya B and Mutalik, Srinivas (2019) Asenapine maleate-loaded nanostructured lipid carriers: optimization and in vitro, ex vivo and in vivo evaluations. Nanomedicine, 14 (7). pp. 889-910. ISSN 1743-5889

[img] PDF
6442 DisplayPdf.pdf - Published Version
Restricted to Registered users only

Download (5MB) | Request a copy

Abstract

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

Item Type: Article
Uncontrolled Keywords: Asenapine maleate; Caco 2 cells; In vivo imaging; Nanostructured lipid carriers
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutics
Depositing User: KMC Library
Date Deposited: 12 Apr 2019 08:53
Last Modified: 12 Apr 2019 08:53
URI: http://eprints.manipal.edu/id/eprint/153653

Actions (login required)

View Item View Item