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.
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