P-toluenesulfonychloride-based niosomes for Amphotericin-B against Leishmaniasis

IF 1.6 4区 工程技术 Q3 CHEMISTRY, APPLIED Journal of Surfactants and Detergents Pub Date : 2024-01-31 DOI:10.1002/jsde.12736
Imdad Ali, Sammer Yousuf, Shafi Ullah, Israr Ali, Mahwish Siddiqui, M. Iqbal Choudhary, Muhammad Raza Shah
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Abstract

Nonionic-surfactants have been reported as nanocarriers for delivering low bioavailable drugs at the target sites. In the current study, two new nonionic surfactants were synthesized to enhance the oral bioavailability of the low water-soluble antifungal drug Amphotericin-B. The hemolysis effect of nonionic surfactants on red blood cells and cytotoxicity against the 3T3 cell line was studied. Both surfactants have shown low hemolysis and cytotoxicity as compared to standard Tween 80. The morphology of drug-loaded niosomes of nonionic surfactants 1 and 2 was studied by using atomic force microscopy (AFM), and both surfactants based vesicles were spherical, while their average sizes were measured by dynamic light scattering (DLS). The average size, zeta potential and polydispersity index (PDI) values of surfactants 1 and 2 were 282 ± 3 nm, −8 ± 1 mV, 0.26 and 287 ± 3 nm, −10 ± 1 mV, 0.24. The drug entrapment efficiency and critical micelle concentrations of nonionic surfactants were determined by using UV–visible spectroscopy. The structures of surfactants 1 and 2 were assessed through single-crystal x-ray crystallographic analysis, while Hirshfeld analysis was performed to study the intermolecular interactions of molecules, as well as the packing behavior of their crystals. The nonionic-surfactant 1 was further tested for antileishmanial activity against Leishmania tropica promastigotes, in both drug-loaded and unloaded niosomal vesicular forms. The nonionic surfactant 1 was found to be a potentanti-leishmanial agent in the drug-loaded form with IC50 = 3.02 ± 0.91 μM in comparison to their standard drugs Amphotericin-B (IC50 = 3.8 ± 0.04 μM) and miltefosine (IC50 = 42.2 ± 0.6 μM) (p < 0.1). These results, therefore, form the basis of further results towards efficient drug delivery against tropical disease Leishmaniasis.

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基于对甲苯磺酸的抗利什曼病两性霉素-Biosomes
据报道,非离子表面活性剂可作为纳米载体将生物利用度较低的药物输送到目标部位。本研究合成了两种新型非离子表面活性剂,以提高低水溶性抗真菌药物两性霉素-B 的口服生物利用度。研究了非离子表面活性剂对红细胞的溶血作用以及对 3T3 细胞系的细胞毒性。与标准吐温 80 相比,两种表面活性剂的溶血作用和细胞毒性都较低。使用原子力显微镜(AFM)研究了非离子表面活性剂 1 和 2 的药物负载型iosomes 的形态,发现这两种表面活性剂的囊泡都呈球形,并通过动态光散射(DLS)测量了它们的平均尺寸。表面活性剂 1 和 2 的平均尺寸、zeta 电位和多分散指数(PDI)值分别为 282 ± 3 nm、-8 ± 1 mV、0.26 和 287 ± 3 nm、-10 ± 1 mV、0.24。利用紫外可见光谱测定了非离子表面活性剂的药物夹带效率和临界胶束浓度。通过单晶 X 射线晶体学分析评估了表面活性剂 1 和 2 的结构,并通过 Hirshfeld 分析研究了分子间的相互作用及其晶体的堆积行为。研究人员还进一步测试了非离子表面活性剂 1 在药物负载和非负载纳米囊泡形态下对热带利什曼原虫的抗利什曼活性。结果发现,与标准药物两性霉素-B(IC50 = 3.8 ± 0.04 μM)和米替福辛(IC50 = 42.2 ± 0.6 μM)相比,非离子表面活性剂 1 是一种有效的载药型抗利什曼病剂,IC50 = 3.02 ± 0.91 μM(p <0.1)。因此,这些结果为进一步研究针对热带疾病利什曼病的高效给药奠定了基础。
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来源期刊
Journal of Surfactants and Detergents
Journal of Surfactants and Detergents 工程技术-工程:化工
CiteScore
3.80
自引率
6.20%
发文量
68
审稿时长
4 months
期刊介绍: Journal of Surfactants and Detergents, a journal of the American Oil Chemists’ Society (AOCS) publishes scientific contributions in the surfactants and detergents area. This includes the basic and applied science of petrochemical and oleochemical surfactants, the development and performance of surfactants in all applications, as well as the development and manufacture of detergent ingredients and their formulation into finished products.
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Issue Information Special issue: Industrial surfactants R&D—A tribute to George A. Smith Issue Information Cloning, purification, and functional characterization of recombinant pullulanase from Bacillus cereusATCC 14579 for improved detergent performance Special Issue: Glycolipid biosurfactants: Synthesis, properties, and applications
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