Enhancement the oral bioavailability of praziquantel by incorporation into solid lipid nanoparticles
The aim of this study was to assess the feasibility of solid lipid nanoparticles (SLN) to enhance the oral bioavailability of praziquantel (PZQ). SLN loaded with PZQ were produced by ultrasound technique. The characteristics of PZQ-SLN were studied in detail. The concentration of PZQ
in plasma was determined using reversed-phase high-performance liquid chromatography after oral administration of PZQ-SLN and control PZQ tablets (PZQ-TAB) in rats respectively. The results showed that PZQ-SLN had an average diameter 110 nm with Zeta potential of –66.3 mV. The encapsulation
efficiency of PZQ was about 80%. In vitro drug release fitted the Weibull distribution equation. There were two peaks in the PZQ concentration-time curves in plasma after oral administration of PZQ-SLN. The first peak might be caused by free drug and that adsorbed onto the surface
of PZQ-SLN. The second peak was indicative of gut uptake of PZQ-SLN. The AUC0→∞ value of PZQ after oral administration of SLN was 4.1 fold higher than that obtained with the PZQ-TAB. The MRT of PZQ-SLN was also significantly enhanced, resulting in an about twofold increase
compared with PZQ-TAB. Thus, the oral bioavailability of PZQ-SLN increased significantly compared to PZQ-TAB, and the results indicate that SLN can be a promising drug carrier for PZQ.
Document Type: Research Article
Affiliations: 1: Department of Pharmaceutics, Shenyang Pharmaceutical University, Wenhua Road 03, Shenyang, 110016, China, Email: [email protected] 2: Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, China
Publication date: 01 February 2009
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