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Journal of Nanotechnology
Volume 2014 (2014), Article ID 351693, 12 pages
http://dx.doi.org/10.1155/2014/351693
Research Article

Intestinal Lymphatic Delivery of Praziquantel by Solid Lipid Nanoparticles: Formulation Design, In Vitro and In Vivo Studies

Department of Pharmaceutics, Indian Institute of Technology, (Banaras Hindu University), Varanasi 221 005, India

Received 29 July 2013; Accepted 5 November 2013; Published 19 February 2014

Academic Editor: John A. Capobianco

Copyright © 2014 Amit Mishra et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

The aim of the present work was to design and develop Praziquantal (PZQ) loaded solid lipid nanoparticles (PZQ-SLN) to improve the oral bioavailability by targeting intestinal lymphatic system. PZQ is practically insoluble in water and exhibits extensive hepatic first-pass metabolism. PZQ SLN were composed of triglycerides, lecithin and various aqueous surfactants; were optimized using hot homogenization followed by ultrasonication method. The optimized SLN had particle size of  nm, EE of %. The drug release of PZQ-SLN showed initial burst release followed by the sustained release. Inspite of zeta potential being around −10 mV, the optimized SLN were stable at storage conditions ( °C and °C/ % RH) for six months. TEM study confirmed the almost spherical shape similar to the control formulations. Solid state characterization using differential scanning calorimeter (DSC) and powder X-ray diffraction (PXRD) analysis confirmed the homogeneous distribution of PZQ within the lipid matrix. The 5.81-fold increase in , after intraduodenal administration of PZQ-SLN in rats treated with saline in comparison to rats treated with cycloheximide (a blocker of intestinal lymphatic pathway), confirmed its intestinal lymphatic delivery. The experimental results indicate that SLN may offer a promising strategy for improving the therapeutic efficacy and reducing the dose.