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Ethosomes 和超变形脂质体用于克霉唑透皮给药:比较评估。

Ethosomes and ultradeformable liposomes for transdermal delivery of clotrimazole: A comparative assessment.

机构信息

College of Pharmacy, IPS Academy, A.B. Road, Indore 452012, MP, India.

出版信息

Saudi Pharm J. 2012 Apr;20(2):161-70. doi: 10.1016/j.jsps.2011.10.001. Epub 2011 Oct 31.

Abstract

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.

摘要

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。

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