A novel solid-in-oil nanosuspension for transdermal delivery of diclofenac sodium
A novel solid-in-oil nanosuspension for transdermal delivery of diclofenac sodium
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DOI：
10.1007/s11095-007-9445-7
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发表时间：
2008-04-01
影响因子：
3.7
通讯作者：
Goto, Masahiro
中科院分区：
文献类型：
--
作者：
Piao, Hongyu;Kamiya, Noriho;Goto, Masahiro
目的。我们配制了一种油包固体纳米混悬剂（SONS）作为双氯芬酸钠（DFNa）的新型透皮递送载体。使用尤卡坦微型猪（YMP）皮肤模型评估 SONS 的基本透皮特性。方法。 DFNa-蔗糖芥酸酯（即表面活性剂）复合物是通过形成油包水乳液来制备的。将复合物悬浮在肉豆蔻酸异丙酯（IPM）中形成 SONS。在 Franz 型扩散池中使用全层 YMP 背侧皮肤检查 SONS 的基本透皮特性。悬浮在 IPM 中但未形成复合物的 DFNa 粉末用作对照。评价表面活性剂与DFNa的重量比对DFNa渗透皮肤的影响。结果。通过与蔗糖芥酸形成复合物，DFNa 以纳米级悬浮液的形式成功分散到 IPM 中。与对照相比，由此产生的 SONS 使 DFNa 在 YMP 皮肤上的渗透通量增加了 3.8 倍。 SONS 的尺寸取决于表面活性剂与 DFNa 的重量比。 DFNa渗透率最高的最佳重量比为8.8，此时SONS的平均直径为14.4 nm。结论。 SONS配方可以增强DFNa的经皮吸收。
Purpose. We formulated a solid-in-oil nanosuspension (SONS) as a novel transdermal delivery carrier for diclofenac sodium (DFNa). The basic transdermal characteristics of the SONS were evaluated using a Yucatan micropig (YMP) skin model.Methods. DFNa-sucrose erucate (i.e. surfactant) complexes were prepared via the formation of a water-in-oil emulsion. The complexes were suspended in isopropyl myristate (IPM) to form a SONS. The basic transdermal characteristics of the SONS were examined using full-thickness YMP dorsal skin in a Franz-type diffusion cell. DFNa powder suspended in IPM without complex formation was used as a control. The effect of the weight ratio of surfactant to DFNa on DFNa penetration of the skin was evaluated.Results. DFNa was successfully dispersed into IPM as a nanosized suspension via complex formation with sucrose erucate. The resultant SONS increased the permeability flux of DFNa across the YMP skin by up to 3.8-fold compared with the control. The size of the SONS depended on the weight ratio of the surfactant to DFNa. The optimal weight ratio for the highest DFNa permeation was 8.8, at which point the mean diameter of the SONS was 14.4 nm.Conclusion. The SONS formulation can enhance the percutaneous absorption of DFNa.