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Int J Pharm ; 516(1-2): 158-169, 2017 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-27989821

RESUMEN

Curcumin (CUR) has a wide spectrum of biological and pharmacological activities, yet problems of its bioavailability remained a major challenge in preclinical studies. Thus, the design of the delivery systems with CUR as a model drug featuring dual release process - an initial burst followed by sustained release - to provide the optimal drug pharmacokinetics in the therapeutic region has been actively pursued. In this study, the 3-aminopropyltriethoxysilane (APTES)-functionalized electrospun poly(N-vinyl-2-pyrrolidone) fibers (NH2-PVP) were utilized as a free-standing substrate for the immobilization of CUR-PVP capped gold nanoparticles (CUR-PGNPs) conjugates. The conjugate was synthesized by sonication and the drug entrapment percentage was determined to be 54.2 ±1.8. CUR-PGNPs immobilized on NH2-PVP fibers showed a moderate burst release during the first few hours, followed by a sustained release lasting for 2days. The drug release was found pH-dependent (pH 5.0>6.0>7.4). The two-stage release profiles of CUR-PGNPs@NH2-PVP fibers were fitted well to Korsmeyer-Peppas model, indicating a non-Fickian diffusion mechanism for initial burst release and Fickian diffusion-controlled mechanism for the sustained release. Initial biocompatibility assessments based on lactate dehydrogenase (LDH) assay and morphological examination by SEM with L-929 mouse fibroblasts revealed that CUR-PGNPs@NH2-PVP nanofibrous scaffold was capable of supporting cell growth over a culture period of 3days.


Asunto(s)
Curcumina/administración & dosificación , Sistemas de Liberación de Medicamentos , Nanopartículas del Metal , Propilaminas/química , Silanos/química , Animales , Línea Celular , Química Farmacéutica/métodos , Curcumina/química , Preparaciones de Acción Retardada , Liberación de Fármacos , Fibroblastos/metabolismo , Oro , Concentración de Iones de Hidrógeno , L-Lactato Deshidrogenasa/metabolismo , Ratones , Polivinilos/química , Pirrolidinas/química , Factores de Tiempo
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