Artículos de revistas
Loading of praziquantel in the crystal lattice of solid lipid nanoparticles Studies by DSC and SAXS
Fecha
2012-04-01Registro en:
Journal of Thermal Analysis and Calorimetry. Dordrecht: Springer, v. 108, n. 1, p. 353-360, 2012.
1388-6150
10.1007/s10973-011-1871-4
WOS:000302704500048
8498310891810082
0000-0002-7984-5908
Autor
Fernando Pessoa Univ
Universidade Estadual Paulista (Unesp)
Univ Tras Os Montes & Alto Douro
Ctr Res & Technol Agroenvironm & Biol Sci
Universidade Federal de Sergipe (UFS)
Univ Tras Os Montes & Alto Douro IBB CGB UTAD
Institución
Resumen
Praziquantel (PZQ) is the drug of choice for oral treatment of schistosomiasis and other fluke infections that affect humans. Its low oral bioavailability demands the development of innovative strategies to overcome the first pass metabolism. In this article, solid lipid nanoparticles loaded with PZQ (PZQ-SLN) were prepared by a modified oil-in-water microemulsion method selecting stearic acid as lipid phase after solubility screening studies. The mean particle size (Z-Ave) and zeta potential (ZP) were 500 nm and -34.0 mV, respectively. Morphology and shape of PZQ-SLN were analysed by scanning electron microscopy revealing the presence of spherical particles with smooth surface. Differential scanning calorimetry suggested that SLN comprised a less ordered arrangement of crystals and the drug was molecularly dispersed in the lipid matrix. No supercooled melts were detected. The entrapment efficiency (EE) and loading capacity of PZQ, determined by high performance liquid chromatography, were 99.06 +/- 0.3 and 17.48 +/- 0.05, respectively. Effective incorporation of PZQ into the particles was confirmed by small angle X-ray scattering revealing the presence of a lipid lamellar structure. Stability parameters of PZQ-SLN stored at room temperature (25 degrees C) and at 4 degrees C were checked by analysing Z-Ave, ZP and the EE for a period of 60 days. Results showed a relatively long-term physical stability after storage at 4 degrees C, without drug expulsion.