Synthesis of novel biocompatible resorcinarene based nanosized dendrimer-vesicles for enhanced anti-bacterial potential of quercetin

Abstract

Resorcinarene based macrocycles has attained remarkable attention in the field of drug delivery because of their self-assembly and unique topology. The current work is based on the synthesis of new resorcinarene based macrocycle (Benzyloxy Macrocycle, BM) to enhance the therapeutic efficacy of quercetin (QRT). The synthesized BM was characterized through Mass, 1H NMR, 13C NMR and FT-IR spectroscopy and investigated for their biocompatibility using cytotoxicity and hemolysis assays. The critical concentration of association (CCA) of BM was determined using UV-Vis Spectrophotometer. The QRT loaded BM dendrimer based nano-vesicles were characterized for size, poly dispersity index (PDI), zeta potential and surface morphology. The anti-bacterial potential of QRT loaded dendrimersomes were studied against multi drug resistant (MDR) S. aureus. The results of the study revealed that the synthesized compound was highly biocompatible as less hemolysis and cytotoxicity was observed. The QRT loaded vesicles revealed smaller size of around 225.5 ± 16.31 nm with 88 ± 1.52% encapsulation of QRT with controlled and sustained drug release profile. The MIC value of QRT significantly decreased to136 µg/mL after being encapsulated in BM nano-vesicles. The antibacterial efficacy of QRT loaded BM nano-vesicles was further authenticated by the AFM images which showed the complete distortion of cell surface morphology of bacteria. Findings of this research work suggest that the synthesized resorcinarene macrocycle have the ability to enhance the therapeutic potential of QRT.