Drug-in-cyclodextrin-in-polymeric nanoparticles: A promising strategy for rifampicin administration

Eur J Pharm Biopharm. 2022 Nov:180:190-200. doi: 10.1016/j.ejpb.2022.10.001. Epub 2022 Oct 7.


The aim of this work was to develop novel chitosan (CH) based nanoparticles (NPs) for rifampicin (RIF) delivery. RIF, a lipophilic molecule, was incorporated inside NPs as a complex with an anionic cyclodextrin, sulphobutyl-ether-β-cyclodextrin (SBE-β-CD). NPs were then prepared through the ionic gelation method by exploiting the interaction between CH and SBE-β-CD-RIF complex (CH/SBE-β-CD-RIF NPs), possibly in the presence of other crosslinkers, like carboxymethylcellulose (CH/SBE-β-CD-RIF/CMC NPs) and pentasodium tripolyphosphate (CH/SBE-β-CD-RIF/TPP NPs). NPs were then characterized for their size, ζ-potential, morphology, yield, drug loading, stability, mucoadhesion, in vitro drug release and antimicrobial activity. Results demonstrated that the functional properties of loaded NPs, like their size, ζ-potential, and stability, varied on the basis of the CH/crosslinker weight ratio. Interestingly, all the developed NPs had a round shape and were characterized by high yield values and mucoadhesive properties. Among them, NPs based on CH/SBE-β-CD-RIF and CH/SBE-β-CD-RIF/CMC have gained high drug loading, provided a sustained release of RIF and showed the best antimicrobial activity. Thus, both types of NPs may be considered as promising nanocarriers for the release of RIF.

Keywords: Antimicrobial activity; Chitosan; Mucoadhesion; Nanoparticles; Rifampicin; Sulphobutyl-ether-β-cyclodextrin.

MeSH terms

  • Anti-Infective Agents*
  • Chitosan*
  • Cyclodextrins*
  • Drug Carriers
  • Nanoparticles*
  • Particle Size
  • Polymers
  • Rifampin / pharmacology


  • Cyclodextrins
  • Rifampin
  • Chitosan
  • Polymers
  • Drug Carriers
  • Anti-Infective Agents