Encapsulation of dexamethasone into biodegradable polymeric nanoparticles

Gomez-Graete, C; Tsapis, N; Besnard M.; Bochot, A; Fattal, E


The present paper concerns both the optimization of dexamethasone (DXM) entrapment and its release from biodegradable poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles prepared by the solvent evaporation process. Since the addition of DXM induced the formation of drug crystals beside the nanoparticle suspension, the influence of several parameters on DXM encapsulation was investigated such as the type of organic solvent and polymer, the DXM initial mass, the evaporation rate of the solvent, the continuous phase saturation and the incorporation of a lipid in the polymer. Nanoparticle size and zeta potential were not modified in the presence of DXM and were respectively around 230 nm and -4 mV. The highest drug loading was obtained using 100 mg PLGA 75:25 in a mixture of acetone-dichloromethane 1:1 (v:v) and 10 mg of DXM. The drug was completely released from this optimized formulation after 4 h of incubation at 37 °C. Neither the evaporation rate of the organic solvent, nor the aqueous phase saturation with salt or the incorporation of 1 mg 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) within the nanoparticles modified the encapsulation efficiency. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) demonstrated that the drug was molecularly dispersed within the nanoparticles whereas the non-encapsulated DXM crystallized. These results demonstrate the feasibility of encapsulating dexamethasone and its subsequent delivery. © 2006 Elsevier B.V. All rights reserved.

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Título según WOS: Encapsulation of dexamethasone into biodegradable polymeric nanoparticles
Título según SCOPUS: Encapsulation of dexamethasone into biodegradable polymeric nanoparticles
Volumen: 331
Número: 2
Editorial: Elsevier
Fecha de publicación: 2007
Página de inicio: 153
Página final: 159
Idioma: English
URL: http://linkinghub.elsevier.com/retrieve/pii/S0378517306009859