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用于局部给药的载硝酸咪康唑固体脂质纳米粒的制备与评价

Preparation and evaluation of miconazole nitrate-loaded solid lipid nanoparticles for topical delivery.

作者信息

Bhalekar Mangesh R, Pokharkar Varsha, Madgulkar Ashwini, Patil Nilam, Patil Nilkanth

机构信息

AISSMS College of Pharmacy, Kennedy Road, Pune, India.

出版信息

AAPS PharmSciTech. 2009;10(1):289-96. doi: 10.1208/s12249-009-9199-0. Epub 2009 Mar 18.

Abstract

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.

摘要

本研究的目的是制备负载硝酸咪康唑(MN)的固体脂质纳米粒(MN-SLN),用于硝酸咪康唑的局部给药。采用Compritol 888 ATO作为脂质,丙二醇(PG)来增加药物在脂质中的溶解度,吐温80和单硬脂酸甘油酯作为表面活性剂,通过热均质法制备MN-SLN分散体,以稳定SLN分散体。SLN分散体的平均粒径在244至766nm之间。所有分散体的包封率都很高,在80%至100%之间。选择了在1个月内表现出良好稳定性的MN-SLN分散体。对该MN-SLN进行了粒径、包封率和X射线衍射表征。使用Franz扩散池对以所选MN-SLN分散体制备的凝胶中硝酸咪康唑在尸体皮肤中的渗透进行了体外评估。差示扫描量热法(DSC)结果表明,MN以无定形状态分散在SLN中。与市售凝胶相比,MN-SLN制剂可显著增加MN在皮肤中的累积摄取,并显示出显著增强的皮肤靶向作用。这些结果表明,所研究的具有皮肤靶向性的MN-SLN制剂可能是硝酸咪康唑局部给药的一种有前景的载体。

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