Synthesis and characterization of thiol modified beta cyclodextrin, its biocompatible analysis and application as a modified release carrier of ticagrelor

Biomed Mater. 2020 Dec 18;16(1):015023. doi: 10.1088/1748-605X/abbf05.

Abstract

Thiol modification of beta cyclodextrin (β-CD) was carried out using thiourea, which served as a thiol donor. The chemical reaction was mediated using HCl. Polymer prepared via thiolation was further subjected to physicochemical and biocompatible analysis. Acute oral toxicity and compatibility was determined in albino rats. Furthermore, compressed tablets of ticagrelor (TCG) were prepared using modified and unmodified polymers and evaluated via various quality control tests. Thiolation was successfully achieved and confirmed by the FTIR scan, as a significant corresponding peak was observed at 2692 cm-1 wavenumber, demonstrating the attachment of -SH group. In vivo analysis has confirmed the safe use of β-CD, as none of the vital organs showed any kind of toxic effects. Dissolution studies revealed that Tβ-CD was able to release 96.62% of the drug within 1 h of the study, hence providing an immediate release. Conclusively, a thiol moiety was successfully attached to the polymeric backbone and was found safe to be used as a pharmaceutical excipient.

MeSH terms

  • Administration, Oral
  • Animals
  • Biocompatible Materials / chemical synthesis
  • Biocompatible Materials / chemistry
  • Biocompatible Materials / toxicity
  • Drug Carriers / chemical synthesis*
  • Drug Carriers / chemistry*
  • Drug Carriers / toxicity
  • Drug Delivery Systems
  • Materials Testing
  • Polymers / chemical synthesis
  • Polymers / chemistry
  • Polymers / toxicity
  • Rats
  • Tablets
  • Thiosugars / chemical synthesis
  • Thiosugars / chemistry
  • Thiosugars / toxicity
  • Thiourea / chemistry
  • Ticagrelor / administration & dosage*
  • beta-Cyclodextrins / chemical synthesis*
  • beta-Cyclodextrins / chemistry*
  • beta-Cyclodextrins / toxicity

Substances

  • Biocompatible Materials
  • Drug Carriers
  • Polymers
  • Tablets
  • Thiosugars
  • beta-Cyclodextrins
  • Ticagrelor
  • Thiourea