Verreck Geert, Chun Iksoo, Rosenblatt Joel, Peeters Jef, Dijck Alex Van, Mensch Jurgen, Noppe Marc, Brewster Marcus E
Johnson & Johnson Pharmaceutical Research and Development, Pharmaceutical Sciences, Drug Evaluation, Turnhousteweg 30, 2340 Beerse, Belgium.
J Control Release. 2003 Oct 30;92(3):349-60. doi: 10.1016/s0168-3659(03)00342-0.
Electrostatic spinning was applied to the preparation of drug-laden nonbiodegradable nanofiber for potential use in topical drug administration and wound healing. The specific aim of these studies was to assess whether these systems might be of interest as delivery systems for poorly water-soluble drugs. Itraconazole and ketanserin were selected as model compounds while a segmented polyurethane (PU) was selected as the nonbiodegradable polymer. For both itraconazole and ketanserin, an amorphous nanodispersion with PU was obtained when the drug/polymer solutions were electrospun from dimethylformide (DMF) and dimethylacetamide (DMAc), respectively. The collected nonwoven fabrics were shown to release the drugs at various rates and profiles based on the nanofiber morphology and drug content. Data were generated using a specially designed release apparatus based around a rotating cylinder. At low drug loading, itraconazole was released from the nanofibers as a linear function of the square root of time suggesting Fickian kinetics. No initial drug burst was observed. A biphasic release pattern was observed for ketanserin in which two sequential linear components were noted. These release phases may be temporally correlated with (1) drug diffusion through the polymer and (2) drug diffusion through formed aqueous pores.
静电纺丝被应用于制备载药的不可生物降解纳米纤维,以用于局部给药和伤口愈合。这些研究的具体目的是评估这些系统作为难溶性药物递送系统是否具有吸引力。选择伊曲康唑和酮色林作为模型化合物,同时选择一种嵌段聚氨酯(PU)作为不可生物降解聚合物。对于伊曲康唑和酮色林,当分别从二甲基甲酰胺(DMF)和二甲基乙酰胺(DMAc)中静电纺丝药物/聚合物溶液时,均获得了与PU的无定形纳米分散体。基于纳米纤维形态和药物含量,所收集的无纺布显示出以不同速率和模式释放药物。数据是使用基于旋转圆筒的专门设计的释放装置生成的。在低药物载量下,伊曲康唑从纳米纤维中释放,其与时间的平方根呈线性关系,表明符合菲克动力学。未观察到初始药物突释。酮色林观察到双相释放模式,其中注意到两个连续的线性成分。这些释放阶段可能在时间上与(1)药物通过聚合物的扩散和(2)药物通过形成的水孔的扩散相关。