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Acta Pharmaceutica Sinica ; (12): 761-765, 2008.
Artículo en Chino | WPRIM | ID: wpr-277799

RESUMEN

This paper described the preparation and liver targeting traits of new solid lipid nanoparticles (SLN) containing floxuridinyl dibutyrate (FUDRB) modified with beta-D-galactosides (G2). FUDRB-SLN and FUDRB-G2SLN were prepared by thin layer ultrasonic technique. Transmission electron microscopy micrograph analysis demonstrated that the particle sizes of FUDRB-SLN and FUDRB-G2SLN were (137.5 +/- 11.1) nm and (95.0 +/- 10.7) nm. Drug loading were 9.64% and 8.56%, and entrapment efficiency were 99.81% and 96.23%, respectively. The concentrations of floxuridine (FUDR) in serum and some organs (liver, kidney and lung) were determined by RP-HPLC after iv administration of SLN. FUDR release was confirmed, and a significant enrichment of SLN modified with G2 was observed in liver with G2 complex (targeting rates of SLN-G2 was 8.28 for liver) in comparison with FUDR-sol (targeting rate was 2.56). FUDR could be detected in liver in mice at 480 min after iv administration of FUDRB-G2SLN. These results suggested that incorporation of G2 (4%-5%, g/g) into SLN enhanced the liver targeting-ability of FUDRB. SLN containing G2 could be a useful drug carrier system for liver targeting.


Asunto(s)
Animales , Femenino , Masculino , Ratones , Antimetabolitos Antineoplásicos , Farmacocinética , Área Bajo la Curva , Portadores de Fármacos , Composición de Medicamentos , Sistemas de Liberación de Medicamentos , Floxuridina , Sangre , Farmacocinética , Galactósidos , Química , Lípidos , Química , Hígado , Metabolismo , Nanopartículas , Tamaño de la Partícula , Distribución Tisular
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