Preparation of doxorubicin-loaded stealth liposomes modified with RGD mimetic and cellular association in vitro / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1085-1090, 2005.
Artículo
en Chino
| WPRIM
| ID: wpr-253526
ABSTRACT
<p><b>AIM</b>To investigate the possibility of using stealth liposomes modified with arginine-glycine-aspartic acid (RGD) mimetic as the targeted carriers to achieve increased accumulation in tumor and enhanced intracellular delivery for the encapsulated anticancer drugs.</p><p><b>METHODS</b>RGD mimetic (RGDm) as a ligand for integrins was synthesized and covalently conjugated to the active PEGylated phospholipids (DSPE-PEG-BTC) to form RGDm conjugate (DSPE-PEG-RGDm). Then RGDm-modified SL (RGDm-SL) containing DOX (RGDm-SL-DOX) and SL containing DOX (SL-DOX) were prepared by film dispersion followed by ammonium sulfate gradient method. The pH-sensitive probe, BCECF-AM, was used to study the binding of melanoma cells to DSPE-PEG-RGDm. Flow cytometry and confocal microscopy were performed to evaluate the cellular association or DOX uptake for RGDm-SL-DOX or SL-DOX in vitro.</p><p><b>RESULTS</b>The melanoma cells A375 and B16 showed enhanced binding to the immobilized DSPE-PEG-RGDm. The cells treated with RGDm-SL-DOX showed remarkable increase in cellular association or DOX uptake compared with SL-DOX.</p><p><b>CONCLUSION</b>The RGDm-modified SL could be as the targeted carriers to facilitate the delivery of the encapsulated anti-cancer drugs into tumor cells by receptor-mediated way.</p>
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Oligopéptidos
/
Patología
/
Fosfatidiletanolaminas
/
Polietilenglicoles
/
Melanoma Experimental
/
Portadores de Fármacos
/
Doxorrubicina
/
Adhesión Celular
/
Núcleo Celular
/
Sistemas de Liberación de Medicamentos
Límite:
Animales
/
Humanos
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2005
Tipo del documento:
Artículo
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