Hassan Eman M, Rabee Ahmed R, Soliman Saied M, Hagar Mohamed, Moneer Esraa A, Ramadan Sherif, Barakat Assem, Abdel-Hamid Hamida, Zakaria Ahmed, Rasheed Hanaa A
Chemistry Department, Faculty of Science, Alexandria University, P.O. Box 426, Alexandria 21321, Egypt.
Department of Medical Laboratory Technology, Faculty of Applied Health Sciences Technology, Pharos University in Alexandria, Alexandria 21500, Egypt.
ACS Omega. 2025 May 15;10(20):20226-20235. doi: 10.1021/acsomega.4c10965. eCollection 2025 May 27.
In the creation of medicine delivery systems, nanotechnology has become an innovator, especially for organic compounds. The manipulation of materials at the nanoscale (1-100 nm) allows for unique physicochemical properties that can enhance the efficacy and bioavailability of therapeutic agents. The objective of the current research is to synthesize the hydrazones nanoparticles which utilizes the ionic gelation method via chitosan as a matrix, and their size was measured via both scanning (SEM) and transmission (TEM) electronic microscopes. Interestingly, the formulated nanoparticles are found to be relatively stable, with a positive net charge and high entrapment efficiency up to 82.6%. The studied compounds were further subjected to molecular docking in the active site of protein TgCDPK1, Lipinski's rule, and Swiss ADMET filter, which showed greater activity for all hydrazones . Furthermore, these compounds were tested for their parasitological activity. The results revealed that the nanoformulation of synthesized hydrazones had great activity against Toxoplasma infection compared to the synthesized hydrazone . Moreover, in brain homogenates from mice infected with Toxoplasma, the nanoformulation demonstrated a noteworthy (64%) decrease in the percentage of cyst burden, which is more effective compared to hydrazone (49%).
在药物递送系统的创建中,纳米技术已成为创新者,尤其是对于有机化合物而言。在纳米尺度(1-100纳米)对材料进行操控可实现独特的物理化学性质,从而提高治疗剂的疗效和生物利用度。当前研究的目的是合成腙纳米颗粒,该纳米颗粒通过以壳聚糖为基质的离子凝胶化方法制备,其尺寸通过扫描电子显微镜(SEM)和透射电子显微镜(TEM)进行测量。有趣的是,所制备的纳米颗粒相对稳定,具有正净电荷且包封率高达82.6%。所研究的化合物进一步在蛋白TgCDPK1的活性位点进行分子对接、应用Lipinski规则以及通过瑞士ADMET过滤器筛选,结果表明所有腙类化合物均具有更高的活性。此外,还对这些化合物的寄生虫学活性进行了测试。结果显示,与合成的腙相比,合成腙的纳米制剂对弓形虫感染具有更强的活性。此外,在感染弓形虫的小鼠脑匀浆中,纳米制剂使囊肿负荷百分比显著降低(64%),这比腙(49%)更有效。