Paseban Kamal, Noroozi Sama, Gharehcheloo Rokhshad, Haddadian Abbas, Falahi Robattorki Farnoush, Dibah Hedieh, Amani Reza, Sabouri Fatima, Ghanbarzadeh Erfan, Hajrasouiha Shadi, Azari Arezou, Rashidian Tina, Mirzaie Amir, Pirdolat Zahra, Salarkia Massoumeh, Shahrava Dorsa Sadat, Safaeinikjoo Fatemeh, Seifi Atena, Sadat Hosseini Niusha, Saeinia Niloofar, Bagheri Kashtali Aliasghar, Ahmadiyan Ali, Mazid Abadi Roza, Sadat Kermani Faezeh, Andalibi Romina, Chitgarzadeh Arman, Tavana Aryan Aryan, Piri Gharaghie Tohid
Department of Biology, Zanjan Branch, Islamic Azad University, Zanjan, Iran.
Department of Neurology, University of Utah, Utah, USA.
Heliyon. 2024 Aug 6;10(16):e35651. doi: 10.1016/j.heliyon.2024.e35651. eCollection 2024 Aug 30.
One of the targeted drug delivery systems is the use of nanocarriers, and one of these drug delivery systems is niosome. Niosome have a nano-vesicular structure and are composed of non-ionic surfactants. Objective: In this study, various niosome-encapsulated meropenem formulations were prepared. Subsequently, their antibacterial and anti-biofilm activities were evaluated against methicillin-resistant (MRSA) strains.
The physicochemical properties of niosomal formulations were characterized using a field scanning electron microscope, X-Ray diffraction, Zeta potential, and dynamic light scattering. Antibacterial and anti-biofilm activities were evaluated using broth microdilution and minimum biofilm inhibitory concentration, respectively. In addition, biofilm gene expression analysis was performed using quantitative Real-Time PCR. To evaluate biocompatibility, the cytotoxicity of niosome-encapsulated meropenem in a normal human diploid fibroblast (HDF) cell line was investigated using an MTT assay.
An F1 formulation of niosome-encapsulated meropenem with a size of 51.3 ± 5.84 nm and an encapsulation efficiency of 84.86 ± 3.14 % was achieved. The synthesized niosomes prevented biofilm capacity with a biofilm growth inhibition index of 69 % and significantly downregulated , and gene expression in MRSA strains (p < 0.05). In addition, the F1 formulation increased antibacterial activity by 4-6 times compared with free meropenem. Interestingly, the F1 formulation of niosome-encapsulated meropenem indicated cell viability >90 % at all tested concentrations against normal HDF cells. The results of the present study indicate that niosome-encapsulated meropenem increased antibacterial and anti-biofilm activities without profound cytotoxicity in normal human cells, which could prove useful as a good drug delivery system.
靶向给药系统之一是使用纳米载体,其中一种药物递送系统是脂质体。脂质体具有纳米囊泡结构,由非离子表面活性剂组成。目的:在本研究中,制备了各种脂质体包裹美罗培南的制剂。随后,评估了它们对耐甲氧西林金黄色葡萄球菌(MRSA)菌株的抗菌和抗生物膜活性。
使用场扫描电子显微镜、X射线衍射、Zeta电位和动态光散射对脂质体制剂的物理化学性质进行表征。分别使用肉汤微量稀释法和最小生物膜抑制浓度评估抗菌和抗生物膜活性。此外,使用定量实时PCR进行生物膜基因表达分析。为了评估生物相容性,使用MTT法研究脂质体包裹美罗培南在正常人二倍体成纤维细胞(HDF)细胞系中的细胞毒性。
获得了一种脂质体包裹美罗培南的F1制剂,其尺寸为51.3±5.84nm,包封率为84.86±3.14%。合成的脂质体具有69%的生物膜生长抑制指数,可有效抑制生物膜形成,并显著下调MRSA菌株中的 、 和 基因表达(p<0.05)。此外,与游离美罗培南相比,F1制剂的抗菌活性提高了4至6倍。有趣的是,脂质体包裹美罗培南的F1制剂在所有测试浓度下对正常HDF细胞的细胞活力均>90%。本研究结果表明,脂质体包裹美罗培南可提高抗菌和抗生物膜活性,且对正常人体细胞无明显细胞毒性,有望成为一种良好的药物递送系统。