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article · ACS Omega

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

20252 citationsOpen accessPharos University in Alexandria

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%).

Research topics

  • Computational Drug Discovery Methods
  • Synthesis and bioactivity of alkaloids
  • Synthesis and biological activity

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DOI: 10.1021/acsomega.4c10965

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