The persistent dissemination of resistant bacterial strains is a grave contemporary global impediment in hospital-acquired infections which needs to be mitigated with immediate effect. In particular, infections from pathogenic multidrug-resistant (MDR) Gram-positive bacteria (like Enterococcus faecalis) which are resistant to conventional antibiotic therapy are attracting immediate global attention. Here we report the synthesis of nanoscale hydroxyapatites (HAPs), which are the well known biomimetic ceramic material having needle shaped morphologies. We have encapsulated vancomycin (VAN) within these nanoparticles and have conjugated the targeting ligand (folic acid) by a facile synthesis process in order to enhance the therapeutic efficacy against MDR E. faecalis. These functionalised HAPs are thoroughly characterised by employing field emission scanning electron microscopy (FESEM), powder x-ray diffraction (PXRD), ultraviolet–visible spectroscopy (UV-Vis) and dynamic light-scattering (DLS) techniques. Our results suggest that these functionalised HAPs could successfully transport vancomycin across the cell wall of MDR E. faecalis through endocytosis. The determination of selective antibacterial activity has been envisaged with the help of extensive in-vitro assays like the minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and the generation of reactive oxygen species (ROS). This study vividly establishes that this folic acid conjugated HAPs are promising antibacterial agents against MDR E. faecalis and related pathogenic resistant bacterial strains.
The antibacterial sensitivity of some single, double and triple chain aroylhydrazine against gram positive and gram negative bacteria were performed by disc diffusion method. Most of the compounds showed appreciable antibacterial activity against different gram positive and gram negative bacteria. The single chain hydrazines are more active then double chain and triple chain hydrazine. Among the single chain aroylhydrazines studied only 4-n-hexyloxy benzoyl hydrazine is the most active. The significant activity of 4-n-hexyloxybenzoyl hydrazine and heptyloxybenzoyl hydrazine against gram positive and gram negative bacteria may be (formation of inhibition zone 8 to 22 mm with most of the test bacteria) due to their liophilicity of the bacterial cell membrane. Anti-microbial activity decreases as the number of carbon of single chain hydrazine increases (C6 > C7 > C8 > C9 > C10 single chain hydrazine). Double chain hydrazines (3, 5 or 3, 4) are more active than triple chain hydrazines (3, 5 > 3, 4 > 3, 4, 5 hydrazine). The antibacterial activities of hydrazines are being decreased as their increasing number of side chain.
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