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Preparation and Evaluation of Miconazole Nitrate-Loaded Solid Lipid Nanoparticles for Topical Delivery

机译:咪康唑硝酸盐固体脂质纳米粒的制备及评价

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摘要

The purpose of this study was to prepare miconazole nitrate (MN) loaded solid lipid nanoparticles (MN-SLN) effective for topical delivery of miconazole nitrate. Compritol 888 ATO as lipid, propylene glycol (PG) to increase drug solubility in lipid, tween 80, and glyceryl monostearate were used as the surfactants to stabilize SLN dispersion in the SLN preparation using hot homogenization method. SLN dispersions exhibited average size between 244 and 766 nm. All the dispersions had high entrapment efficiency ranging from 80% to 100%. The MN-SLN dispersion which showed good stability for a period of 1 month was selected. This MN-SLN was characterized for particle size, entrapment efficiency, and X-ray diffraction. The penetration of miconazole nitrate from the gel formulated using selected MN-SLN dispersion as into cadaver skins was evaluated ex-vivo using franz diffusion cell. The results of differential scanning calorimetry (DSC) showed that MN was dispersed in SLN in an amorphous state. The MN-SLN formulations could significantly increase the accumulative uptake of MN in skin over the marketed gel and showed a significantly enhanced skin targeting effect. These results indicate that the studied MN-SLN formulation with skin targeting may be a promising carrier for topical delivery of miconazole nitrate.
机译:这项研究的目的是制备有效地局部递送硝酸咪康唑的负载硝酸咪康唑(MN)的固体脂质纳米颗粒(MN-SLN)。使用Compritol 888 ATO作为脂质,使用丙二醇(PG)提高表面活性剂在脂质中的溶解度,吐温80和单硬脂酸甘油酯作为表面活性剂,以通过热均质法稳定SLN制剂中的SLN分散。 SLN分散体的平均粒径在244至766 nm之间。所有分散体具有80%至100%的高包封率。选择在1个月内显示出良好稳定性的MN-SLN分散体。该MN-SLN的特征在于粒径,截留效率和X射线衍射。使用franz扩散池体外评估了咪康唑硝酸盐从使用选定的MN-SLN分散体配制的凝胶中渗入尸体皮肤的渗透性。差示扫描量热法(DSC)的结果表明,MN以无定形状态分散在SLN中。 MN-SLN制剂可以显着增加市售凝胶中皮肤中MN的累积吸收,并显示出显着增强的皮肤靶向效果。这些结果表明具有皮肤靶向性的所研究的MN-SLN制剂可能是用于局部递送硝酸咪康唑的有希望的载体。

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