College of Pharmacy, IPS Academy, A.B. Road, Indore 452012, MP, India.
Saudi Pharm J. 2012 Apr;20(2):161-70. doi: 10.1016/j.jsps.2011.10.001. Epub 2011 Oct 31.
THE OBJECTIVE OF WORK WAS TO FORMULATE, EVALUATE AND COMPARE THE TRANSDERMAL POTENTIAL OF NOVEL VESICULAR NANOCARRIERS: ethosomes and ultradeformable liposomes, containing clotrimazole (CLT), an anti-fungal bioactive. The ethosomal formulation (ET4) and ultradeformable liposomal (UL) formulation (TT3) showed highest entrapment 68.73 ± 1.4% and 55.51 ± 1.7%, optimal nanometric size range 132 ± 9.5 nm and 121 ± 9.7 nm, and smallest polydispersity index 0.027 ± 0.011 and 0.067 ± 0.009, respectively. The formulation ET4 provided enhanced transdermal flux 56.25 ± 5.49 μg/cm(2)/h and decreased the lag time of 0.9 h in comparison to TT3 formulation (50.16 ± 3.84 μg/cm(2)/h; 1.0 h). Skin interaction and FT-IR studies revealed greater penetration enhancing effect of ET4 than TT3 formulation. ET4 formulation also had the highest zone of inhibition (34.6 ± 0.57 mm), in contrast to TT3 formulation (29.6 ± 0.57 mm) and marketed cream formulation (19.0 ± 1.00 mm) against candidal species. Results suggested ethosomes to be the most proficient carrier system for dermal and transdermal delivery of clotrimazole.
工作的目的是制定、评估和比较新型囊泡纳米载体：醇质体和超变形脂质体，包含克霉唑（CLT），一种抗真菌生物活性物质。醇质体配方（ET4）和超变形脂质体配方（TT3）表现出最高的包封率 68.73±1.4% 和 55.51±1.7%，最佳纳米尺寸范围 132±9.5nm 和 121±9.7nm，最小的多分散指数 0.027±0.011 和 0.067±0.009。与 TT3 配方（50.16±3.84μg/cm(2)/h；1.0h）相比，ET4 配方提供了增强的透皮通量 56.25±5.49μg/cm(2)/h，并减少了滞后时间 0.9h。皮肤相互作用和 FT-IR 研究表明，ET4 配方比 TT3 配方具有更大的渗透增强作用。ET4 配方也具有最高的抑菌区（34.6±0.57mm），与 TT3 配方（29.6±0.57mm）和市售乳膏配方（19.0±1.00mm）相比，对念珠菌有更强的抑制作用。结果表明，醇质体是克霉唑经皮和透皮传递的最有效载体系统。
