Characterization and application of roxithromycin loaded cyclodextrin based nanoparticles for treatment of multidrug resistant bacteria

Mater Sci Eng C Mater Biol Appl. 2016 Apr 1:61:1-7. doi: 10.1016/j.msec.2015.11.076. Epub 2015 Dec 2.

Abstract

An outbreak of infections with a high mortality rate caused by multidrug resistant (MDR) bacteria is one of the biggest health challenges globally. A class IV drug, roxithromycin (ROX), has poor solubility. In this study, ROX was first encapsulated in the cavity of each of the β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD). Then, each of the resulting βCD-ROX inclusion complex and HPβCD-ROX inclusion complex were separately loaded into poly-(lactic-co-glycolic acid) (PLGA) to synthesize βCD-ROX/PLGA and HPβCD-ROX/PLGA nanoparticles (NPs). Blank and ROX loaded PLGA (ROX-PLGA) NPs were also prepared. The loading efficiency of ROX is comparatively high for HPβCD-ROX/PLGA NPs in comparison to the βCD-ROX/PLGA NPs and ROX-PLGA NPs. All designed formulations showed significant (P<0.0001) antibacterial activity against the selected MDR bacterial strains. In a nutshell, this study demonstrated a great therapeutic potential of the above-mentioned delivery systems for treatment of MDR bacteria.

Keywords: Antimicrobial activity; Cyclodextrin; Inclusion complex; Nanoparticles; Poly-(lactic-co-glycolic acid); Roxithromycin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bacteria / growth & development*
  • Cyclodextrins* / chemistry
  • Cyclodextrins* / pharmacology
  • Drug Resistance, Multiple, Bacterial / drug effects*
  • Nanoparticles / chemistry*
  • Roxithromycin* / chemistry
  • Roxithromycin* / pharmacology

Substances

  • Cyclodextrins
  • Roxithromycin