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吲哚美辛经皮给药纳米乳剂的研究:表征、流变学特性及体外皮肤渗透研究

Investigation of true nanoemulsions for transdermal potential of indomethacin: characterization, rheological characteristics, and ex vivo skin permeation studies.

作者信息

Shakeel Faiyaz, Ramadan Wafa, Ahmed Musa A

机构信息

Department of Pharmaceutics, Al-Arab Medical University, Benghazi 5341, Libya.

出版信息

J Drug Target. 2009 Jul;17(6):435-41. doi: 10.1080/10611860902963021.

Abstract

The aim of the present study was to investigate the potential of true nanoemulsions for transdermal delivery of indomethacin. Thermodynamically stable true nanoemulsions were characterized for morphology using transmission electron microscopy (TEM), droplet size, rheological characteristics, and refractive index. The rheological behavior for all true nanoemulsions was found to be Newtonian as viscosity was unchanged by increasing the rate of shear. The ex vivo skin permeation studies were performed using Franz diffusion cell with rat skin as permeation membrane. The ex vivo skin permeation profile of optimized formulation was compared with marketed Indobene gel and nanoemulsion gel. Significant increase in permeability parameters was observed in nanoemulsion formulations (P < 0.05). The steady-state flux (J(ss)) and permeability coefficient (K(p)) for optimized nanoemulsion formulation were found to be 73.96 +/- 2.89 mug/cm(2)/h and 1.479 x 10(-2) +/- 0.289 x 10(- 2 )cm/h, respectively, which were significant compared with Indobene gel and nanoemulsion gel (P < 0.05). Enhancement ratio (E(r)) was found to be 7.88 in optimized formulation F6 compared with other formulations. These results suggested that nanoemulsions can be used as potential vehicles for improved transdermal delivery of indomethacin.

摘要

本研究的目的是探讨真纳米乳剂用于吲哚美辛经皮给药的潜力。使用透射电子显微镜(TEM)、液滴大小、流变学特性和折射率对热力学稳定的真纳米乳剂的形态进行了表征。由于剪切速率增加时粘度不变,发现所有真纳米乳剂的流变行为均为牛顿流体。使用以大鼠皮肤为渗透膜的Franz扩散池进行了体外皮肤渗透研究。将优化制剂的体外皮肤渗透曲线与市售的吲哚美辛凝胶和纳米乳剂凝胶进行了比较。在纳米乳剂制剂中观察到渗透参数显著增加(P<0.05)。优化后的纳米乳剂制剂的稳态通量(J(ss))和渗透系数(K(p))分别为73.96±2.89μg/cm²/h和1.479×10⁻²±0.289×10⁻²cm/h,与吲哚美辛凝胶和纳米乳剂凝胶相比具有显著性差异(P<0.05)。与其他制剂相比,优化后的制剂F6的增强比(E(r))为7.88。这些结果表明,纳米乳剂可用作改善吲哚美辛经皮给药的潜在载体。

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