β-Cyclodextrin complexation as an effective drug delivery system for meropenem

Eur J Pharm Biopharm. 2016 Feb:99:24-34. doi: 10.1016/j.ejpb.2015.10.013. Epub 2015 Nov 22.

Abstract

Following the preparation of an inclusion complex of β-cyclodextrin and meropenem, methods based on FT-IR, Raman and DSC were used for its characterization. An analysis of changes in the stability of meropenem after complexation showed that the complex may serve as a valuable delivery system significantly contributing to enhanced meropenem stability in aqueous solutions and in the solid phase. Due to a sustained transfer of meropenem from the cavity of the cyclodextrin it was possible to maintain a constant desired meropenem concentration over a period of 20 h, as confirmed by a release study. An evaluation of microbial activity not only demonstrated that the bactericidal action of meropenem was not stopped as a result of complexation but even pointed to greater growth inhibition in certain clinically important strains. The fact that investigations of meropenem stability and microbial activity proposed the carbonyl groups as those domains of a meropenem molecule that are instrumental in the formation of a complex with β-cyclodextrin supports the findings of theoretical studies based on molecular modeling.

Keywords: Inclusion complex; Meropenem; Microbiological activity; Solubility; Stability; β-Cyclodextrin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites / physiology
  • Drug Delivery Systems / methods*
  • Macromolecular Substances / administration & dosage
  • Macromolecular Substances / chemistry
  • Macromolecular Substances / metabolism
  • Meropenem
  • Microbial Sensitivity Tests / methods
  • Thienamycins / administration & dosage*
  • Thienamycins / chemistry*
  • Thienamycins / metabolism
  • beta-Cyclodextrins / administration & dosage*
  • beta-Cyclodextrins / chemistry*
  • beta-Cyclodextrins / metabolism

Substances

  • Macromolecular Substances
  • Thienamycins
  • beta-Cyclodextrins
  • Meropenem
  • betadex