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

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-13-cyclodextrin (SBE-13-CD). NPs were then prepared through the ionic gelation method by exploiting the interaction between CH and SBE-13-CD-RIF complex (CH/SBE-13-CD-RIF NPs), possibly in the presence of other crosslinkers, like carboxymethylcellulose (CH/SBE-13-CD-RIF/CMC NPs) and pentasodium tripolyphosphate (CH/ SBE-13-CD-RIF/TPP NPs). NPs were then characterized for their size, zeta-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, zeta-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-13-CD-RIF and CH/SBE-13-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.

Automated summary

This work aimed to develop chitosan-based nanoparticles for the delivery of rifampicin. The nanoparticles were prepared by the ionic gelation method using anionic cyclodextrin as a complex with rifampicin, and other crosslinkers were also used. The nanoparticles were characterized for their properties, and it was found that the loaded nanoparticles showed different functional properties depending on the weight ratio of chitosan and crosslinkers. Among them, nanoparticles based on chitosan with anionic cyclodextrin showed high drug loading, sustained release, and antimicrobial activity, making them promising nanocarriers for drug delivery.