Fabricating Β-cyclodextrin based pH-responsive nanotheranostics as a programmable polymeric nanocapsule for simultaneous diagnosis and therapy

Atefeh Zarepour, Ali Zarrabi*, Kim Lambertsen Larsen

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

15 Citations (Scopus)
40 Downloads (Pure)


Background: Fabrication of a smart drug delivery system that could dramatically increase the efficiency of chemotherapeutic drugs and reduce the side effects is still a challenge for pharmaceutical researchers. By the emergence of nanotechnology, a huge window was opened towards this goal, and a wide type of nanocarriers were introduced for delivering the chemotherapeutic to the cancer cells, among them are cyclodextrins with the ability to host different types of hydrophobic bioactive molecules through inclusion complexation process. Aim: The aim of this study is to design and fabricate a pH-responsive theranostic nanocapsule based on cyclodextrin supramolecular nano-structure. Materials and methods: This nanostructure contains iron oxide nanoparticles in the core surrounded with three polymeric layers including polymeric Β-cyclodextrin, polyacrylic acid conjugated to sulfadiazine, and polyethylenimine functionalized with Β-cyclodextrin. Sulfadiazine is a pH-responsive hydrophobic component capable of making inclusion complex with Β-cyclodextrin available in the first and third layers. Doxorubicin, as an anti-cancer drug model, was chosen and the drug loading and release pattern were determined at normal and acidic pH. Moreover, the biocompatibility of the nanocapsule (with/without drug component) was examined using different techniques such as MTT assay, complement activation, coagulation assay, and hemolysis. Results: The results revealed the successful preparation of a spherical nanocapsule with mean size 43±1.5 nm and negatively charge of -43 mV that show 160% loading efficacy. Moreover, the nanocapsule has an on/off switching release pattern in response to pH that leads to drug released in low acidic pH. The results of the biocompatibility tests indicated that this nano drug delivery system had no effect on blood and immune components while it could affect cancer cells even at very low concentrations (0.3 µg mL-1). Conclusion: The obtained results suggest that this is a “switchable” theranostic nanocapsule with potential application as an ideal delivery system for simultaneous cancer diagnosis and therapy.

Original languageEnglish
JournalInternational Journal of Nanomedicine
Pages (from-to)7017-7038
Number of pages22
Publication statusPublished - 1 Jan 2019


  • Host-guest interaction
  • Nanocapsule
  • On/off switching
  • Ph-responsive
  • Smart nanocarrier


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