Synthesis and Biological Evaluation of Amoxicillin Loaded Hybrid Material Composite Spheres Against Methicillin-Resistant Staphylococcus aureus.

BACKGROUND: Incoherent use of antibiotics has led toward resistance in MRSA, becoming multidrug-resistant with a high rate of virulence in the community and hospital settings. OBJECTIVE: Synergistic anti-MRSA activity was investigated in this study for hybrid material composite spheres of amoxicillin, Ag nanoparticles, and chitosan, which were prepared by one-step synthesis method, and various characterizations were performed. METHODS: Antimicrobial-susceptibility assay on MRSA was achieved by disc diffusion and agar dilution techniques, while agar well diffusion was used for hybrid composite spheres. The in vitro and cytotoxicity studies were conducted on the skin abrasion mouse model and MTT assay on RD cell, respectively. RESULTS: All isolates showed resistance to the tested antibiotics except vancomycin. MIC against MRSA showed high resistance with amoxicillin from 4 to 128 mg L-1. The mean diameter of chitosan spheres and Ag nanoparticles was 02 mm and 277 nm, respectively. Morphology of spheres was uneven, varied, porous, and irregular in SEM, and Ag nanoparticles presence and formation was also seen in the micrograph. No substantial interface among drug, nanoparticles, and polymer was found in XRD, and IR showed characteristic peaks of all compounds in the formulation. The in vitro assay showed augmented anti-MRSA activity with amoxicillin loaded hybrid composite spheres (22-29 mm). A significant reduction in microbial burden (~6.5 log10 CFU mL-1) was seen in vivo with loaded hybrid composite spheres formulation. The MTT assay indicated no potential cytotoxicity with hybrid composite spheres. CONCLUSION: The synergistic effect of Amoxycillin in the current study predicts a promising hybrid formulation with enhanced anti-MRSA activity.

Effect of commercial and green synthesized ZnO NPs in murine model of chloroquine-induced pruritus.

Purpose: To investigate the effects of zinc oxide nanoparticles (ZnO NPs) on chloroquine (CQ)-induced itching, and overall behavior of mice after oral administration of ZnO NPs of various sizes and doses. Background: With the wide-spread use of ZnO NPs in pharmaceuticals and cosmetics, concerns about their safety and toxicity are also increasing. Multiple aspects of ZnO NPs regarding cytotoxicity and tolerability are under investigation globally. Still, a clear conclusion about their safety has not been reached. Chloroquine phosphate is an antimalarial with known side effects of itching in humans and animals. In this study, CQ was used to induce itching in mice, and the effects of ZnO NPs on scratching and other neurological behavior of mice were observed. Methods: Female BALB/c mice were divided into eleven groups of six mice each. ZnO NPs of various sizes and doses were administered orally 1 hour before CQ (32 mg/kg body weight) was administered subcutaneously. The effect of ZnO NPs on CQ-induced pruritus was observed for the next 30 minutes. Simultaneously, overall behavioral changes (socialization and locomotion) were also recorded using a video camera. Results: A significant reduction (P˂0.001) in scratching bouts was observed at all three doses of ZnO NPs (particle sizes 100, 30 nm, and green synthesized 30 nm). Locomotion was reduced significantly (P˂0.001) in ZnO NPs-treated groups in comparison to normal saline and CQ group, additionally, a significant increase in socialization (P˂0.05) was observed in ZnO NP-treated groups as compared to CQ group. Conclusion: ZnO NPs, instead of aggravating the dermatological condition, ameliorated the pruritus. All sizes of ZnO NPs used significantly improved socialization among mice and reduced locomotion activity.

Design, Formulation and In Vitro Evaluation of Sustained-release Tablet Formulations of Levosulpiride.

OBJECTIVES: Levosulpiride is a widely used gastroprokinetic agent in the treatment of various gastric disorders; however, its short half-life and increased dosage frequency leads to non-compliance and possible adverse effects. The prime objective of the current study was to develop a sustained-release formulation of Levosulpiride incorporating bioresorbable cellulose derivatives. MATERIALS AND METHODS: Sustained-release formulations of Levosulpiride were prepared through direct compression using various cellulose derivatives such as CMC sodium, HPC, and HPMC in different polymer-to-drug weight ratios as release-modifying polymers. The powder blends and compressed tablets were then subjected to pre-compressional and post-compressional evaluation, as well as FTIR analysis. In vitro release studies were performed for all formulations of the model drug in buffer solution of pH 6.8 at a wave length of 214 nm by a UV-visible light spectrophotometer. RESULTS: The FTIR results confirmed that the interaction between components was physical, and from the different kinetic models data, the release profile was best expressed by the Higuchi model because the results showed high linearity. The results also showed formulation F9 to be the ideal one among the developed formulations, exhibiting sustained- release behavior. CONCLUSION: Levosulpiride sustained-release matrices were prepared successfully using CMC sodium, HPC, and HPMC as the release-retarding polymer/carrier.

Enhancing the Anti-Enterococci Activity of Different Antibiotics by Combining With Metal Oxide Nanoparticles.

BACKGROUND: Enterococci have emerged as more virulent and multidrug-resistant in community and hospital settings. The emergence of vancomycin resistant enterococci (VRE) in hospitals has posed a serious threat to public health. The widespread use of antibiotics to treat VRE infections has resulted in the development of resistant forms of these organisms. OBJECTIVES: Present study deals with the efficacy of antibiotic-nanoparticle combination against clinical isolates of VRE. This study has effectively evaluated the anti-enterococcal activity of metallic nanoparticles and their combination with antibiotics with the aim to search for new biocidal combinations. MATERIALS AND METHODS: Initially, the isolates were identified by various biochemical tests and also by PCR, targeting ddl, vanA and vanB genes. Antibiotic susceptibility testing was carried out by disc diffusion method. Minimum inhibitory concentration (MIC) of both antibiotics and metal nanoparticles against VRE was done using broth dilution method. On the basis of MICs, a combination of both antibiotics and nanoparticles was used by physical mixing of antibiotics and different concentrations of nanoparticles. RESULTS: The MIC of metal nanoparticles were found in the range of 0.31 - 30 mM. The combination of both antibiotics and nanoparticles has effectively reduced the MICs of ciprofloxacin from 16 - 256 µg/mL to 2 - 16 µg/mL, erythromycin 1024 - 2048 µg/mL to 128 - 512 µg/mL, methicillin 32 - 256 µg/mL to 8 - 64 µg/mL and vancomycin 2 - 512 µg/mL to 0.5 - 64 µg/mL. CONCLUSIONS: Among the nanoparticles, ZnO was found as a potent metallic nanoparticle which effectively reduced the MIC upon combination with the antibiotics. The combination exhibited enhanced bactericidal activity against multidrug resistant clinical strains of VRE with dose dependency. Further extensive study on this aspect can prove their beneficial clinical use against resistant pathogens to combat increasing resistance to antibiotics.