In Vitro Evaluation of Antimicrobial Activity and Cytotoxicity of Different Nanobiotics Targeting Multidrug Resistant and Biofilm Forming Staphylococci

Biomed Res Int. 2018 Nov 28:2018:7658238. doi: 10.1155/2018/7658238. eCollection 2018.

Abstract

Antibiotic-resistant and biofilm-forming bacteria have surprisingly increased over recent years. On the contrary, the rate of development of new antibiotics to treat these emerging superbugs is very slow. Therefore, the aim of this study was to prepare novel nanobiotic formulations to improve the antimicrobial activity of three antibiotics (linezolid, doxycycline, and clindamycin) against Staphylococci. Antibiotics were formulated as nanoemulsions and evaluated for their antimicrobial activities and cytotoxicities. Cytotoxicity of the conventional antibiotics and nanobiotics was analyzed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on rat hepatocytes. Half-maximal inhibitory concentration (IC50) was estimated from an experimentally derived dose-response curve for each concentration using GraphPad Prism software. Upon quantitative assessment of Staphylococcus biofilm formation, eighty-four isolates (66.14 %) were biofilm forming. Linezolid and doxycycline nanobiotics exhibited promising antibacterial activities. On the contrary, clindamycin nanobiotic exhibited poor antibacterial activity. Minimum biofilm inhibitory concentrations showed that 73.68 %, 45.6%, and 5.2% of isolates were sensitive to linezolid, doxycycline, and clindamycin nanobiotics, respectively. Results of this study revealed that antibiotics loaded in nanosystems had a higher antimicrobial activity and lower cytotoxicities as compared to those of conventional free antibiotics, indicating their potential therapeutic values.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / pharmacology*
  • Biofilms / drug effects*
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical / methods
  • Drug Resistance, Multiple, Bacterial / drug effects*
  • Hepatocytes / metabolism
  • Hepatocytes / microbiology
  • Hepatocytes / pathology
  • Rats
  • Software*
  • Staphylococcal Infections / drug therapy*
  • Staphylococcal Infections / metabolism
  • Staphylococcal Infections / pathology
  • Staphylococcus / physiology*

Substances

  • Anti-Bacterial Agents