Evaluation of cell and hemocompatibility of Cucurbiturils

Eur J Pharm Sci. 2020 Apr 15:146:105271. doi: 10.1016/j.ejps.2020.105271. Epub 2020 Feb 19.

Abstract

Background: Cucurbiturils (CB) are pumpkin-shaped macrocyclic molecules consisting of methylen-bridged glycoluril units. Because of their complexing characteristics, they can be used as drug containers for medical purposes. For future biomedical and dermal application of CB, the investigation of cell compatibility is essential. Little is known about the influence of CB on eukaryotic cells, especially on dermal keratinocytes. The structurally related cyclodextrins are known to induce cell death by apoptosis in HaCaT keratinocytes as well as hemolysis in erythrocytes.

Objective: To examine cytotoxic effects of different CB.

Methods: Different cytotoxicity tests were performed on HaCaT keratinocytes and erythrocytes incubated with CB[5], CB[6], and CB[7].

Results: CB[5] and CB[6] did not lead to cytotoxic reactions at high concentrations up to 30 mg/mL whereas incubation with CB[7] triggered apoptosis at a concentration of 3.75 mg/mL. None of the investigated CB caused hemolytic effects on erythrocytes.

Conclusion: These results confirm the high potential of CB as host-complexes for biomedical and dermal applications.

Keywords: Cell viability; Cucurbiturils; Cytotoxicity; Hemolysis.

MeSH terms

  • Apoptosis / drug effects
  • Cells, Cultured
  • Hemolysis / drug effects
  • Humans
  • Keratinocytes / cytology
  • Keratinocytes / drug effects*
  • Macrocyclic Compounds / pharmacology*
  • Skin / drug effects

Substances

  • Macrocyclic Compounds
  • cucurbit(n)uril