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首页> 外文期刊>Saudi Pharmaceutical Journal >Sulfanilamide in solution and liposome vesicles; in vitro release and UV-stability studies
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Sulfanilamide in solution and liposome vesicles; in vitro release and UV-stability studies

机译:溶液和脂质体囊泡中的磺胺;体外释放和紫外线稳定性研究

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The main goal of this study was to develop a liposome formulation with sulfanilamide and to investigate the liposomes impact on its release and stability to the UV-A/UV-B and UV-C irradiation. Liposome dispersions with incorporated sulfanilamide were prepared by thin-film hydration method and liposomes role to the sulfanilamide release was investigated by using a dialysis method. Comparatively, sulfanilamide in phosphate buffer solution was subject to release study as well to the UV irradiation providing for the possibilities of kinetics analysis. In vitro drug release study demonstrated that 20% of sulfanilamide was released from liposomes within 1 h that is approximately twice as slower as in the case of dissolved sulfanilamide in phosphate buffer solution. The kinetic release process can be described by Korsmeyer–Peppas model and according to the value of diffusion release exponent it can be concluded that drug release mechanism is based on the phenomenon of diffusion. The sulfanilamide degradation in phosphate buffer solution and liposomes is related to the formation of UV-induced degradation products that are identified by UHPLC/MS analysis as: sulfanilic acid, aniline and benzidine. The UV-induced sulfanilamide degradation in the phosphate buffer solution and liposome vesicles fits the first- order kinetic model. The degradation rate constants are dependent on the involved UV photons energy input as well as sulfanilamide microenvironment. Liposome microenvironment provides better irradiation sulfanilamide stability. The obtained results suggest that liposomes might be promising carriers for delayed sulfanilamide delivery and may serve as a basis for further research.
机译:这项研究的主要目的是开发一种具有磺胺的脂质体制剂,并研究脂质体对其释放和对UV-A / UV-B和UV-C辐射的稳定性的影响。通过薄膜水化法制备掺入磺胺的脂质体分散体,并通过透析研究脂质体对磺胺释放的作用。相比之下,磷酸盐缓冲溶液中的磺胺也要进行释放研究,同时还要进行紫外线照射,以提供动力学分析的可能性。体外药物释放研究表明,脂质体中20%的磺胺在1小时内释放,其速度是磺胺在磷酸盐缓冲溶液中溶解的速度的两倍。动力学释放过程可以用Korsmeyer-Peppas模型描述,根据扩散释放指数的值可以得出结论,药物释放机理是基于扩散现象的。磷酸盐缓冲溶液和脂质体中磺胺的降解与UV诱导的降解产物的形成有关,通过UHPLC / MS分析将其鉴定为:磺胺酸,苯胺和联苯胺。紫外线诱导的磷酸盐缓冲溶液和脂质体囊泡中磺胺的降解符合一级动力学模型。降解速率常数取决于所涉及的紫外线光子能量输入以及磺胺微环境。脂质体微环境提供了更好的辐照磺胺稳定性。获得的结果表明,脂质体可能是有希望的硫磺酰胺递送延迟载体,并且可以作为进一步研究的基础。

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