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溶液和脂质体囊泡中的磺胺;释放及紫外线稳定性研究。

Sulfanilamide in solution and liposome vesicles; release and UV-stability studies.

作者信息

Petrović Sanja, Tačić Ana, Savić Saša, Nikolić Vesna, Nikolić Ljubiša, Savić Sanela

机构信息

University of Nis - Faculty of Technology, Department of Organic and Technological Sciences, Bulevar Oslobodjenja 124, 16000 Leskovac, Serbia.

University of Belgrade - Faculty of Pharmacy, Department of Pharmaceutical Technology and Cosmetology, Vojvode Stepe 450, 11221 Belgrade, Serbia.

出版信息

Saudi Pharm J. 2017 Dec;25(8):1194-1200. doi: 10.1016/j.jsps.2017.09.003. Epub 2017 Sep 12.

Abstract

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. 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.

摘要

本研究的主要目标是开发一种含有磺胺的脂质体制剂,并研究脂质体对其释放以及对UV-A/UV-B和UV-C辐射稳定性的影响。通过薄膜水化法制备了含有磺胺的脂质体分散体,并采用透析法研究了脂质体对磺胺释放的作用。相比之下,对磷酸盐缓冲溶液中的磺胺也进行了释放研究以及UV辐射研究,以便进行动力学分析。药物释放研究表明,1小时内20%的磺胺从脂质体中释放出来,这比溶解在磷酸盐缓冲溶液中的磺胺释放速度慢约两倍。动力学释放过程可用Korsmeyer-Peppas模型描述,根据扩散释放指数的值可以得出药物释放机制基于扩散现象。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分析鉴定为:磺胺酸、苯胺和联苯胺。磷酸盐缓冲溶液和脂质体囊泡中UV诱导的磺胺降解符合一级动力学模型。降解速率常数取决于所涉及的UV光子能量输入以及磺胺的微环境。脂质体微环境提供了更好的磺胺辐射稳定性。所得结果表明,脂质体可能是用于延迟磺胺递送的有前景的载体,并可为进一步研究提供基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/99e4/6111141/487455e17b6a/gr1.jpg

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