Nanoformulations for Hydrazones; Synthesis, Characterization, Parasitology, and Histopathology Investigations

腙类化合物的纳米制剂;合成、表征、寄生虫学和组织病理学研究

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Abstract

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 3-(a*-c*) 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 3-(a-c). Furthermore, these compounds were tested for their parasitological activity. The results revealed that the nanoformulation of synthesized hydrazones 3-(a*-c*) had great activity against Toxoplasma infection compared to the synthesized hydrazone 3-(a-c). Moreover, in brain homogenates from mice infected with Toxoplasma, the nanoformulation 3c* demonstrated a noteworthy (64%) decrease in the percentage of cyst burden, which is more effective compared to hydrazone 3c (49%).

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