title: β-Cyclodextrin complexation as an effective drug delivery system for meropenem.
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.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Poznan University of Medical Sciences, Grunwaldzka 6, 60-780 Poznan, Poland.
authors.forename: Magdalena
authors.initials: M
authors.lastname: Paczkowska
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Poznan University of Medical Sciences, Grunwaldzka 6, 60-780 Poznan, Poland.
authors.forename: Mikołaj
authors.initials: M
authors.lastname: Mizera
authors.affiliation: Department of Biotechnology and Food Microbiology, Poznan University of Life Sciences, Wojska Polskiego 48, 60-627 Poznan, Poland.
authors.forename: Daria
authors.initials: D
authors.lastname: Szymanowska-Powałowska
authors.affiliation: Department of Molecular Crystals, Institute of Molecular Physics, Polish Academy of Sciences, Smoluchowskiego 17, 60-179 Poznan, Poland.
authors.forename: Kornelia
authors.initials: K
authors.lastname: Lewandowska
authors.affiliation: Institute of Animal Reproduction and Food Research of Polish Academy of Sciences, Tuwima 10, 10-748 Olsztyn, Poland.
authors.forename: Wioletta
authors.initials: W
authors.lastname: Błaszczak
authors.affiliation: Faculty of Chemistry, Adam Mickiewicz University in Poznan, Umultowska 89b, 61-614 Poznan, Poland.
authors.forename: Joanna
authors.initials: J
authors.lastname: Gościańska
authors.affiliation: Faculty of Chemistry, Adam Mickiewicz University in Poznan, Umultowska 89b, 61-614 Poznan, Poland.
authors.forename: Robert
authors.initials: R
authors.lastname: Pietrzak
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Poznan University of Medical Sciences, Grunwaldzka 6, 60-780 Poznan, Poland. Electronic address: jpiontek@ump.edu.pl.
authors.forename: Judyta
authors.initials: J
authors.lastname: Cielecka-Piontek
mesh_terms: D001665:Binding Sites / Q000502:physiology; D016503:Drug Delivery Systems / Q000379:methods*; D046911:Macromolecular Substances / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D000077731:Meropenem; D008826:Microbial Sensitivity Tests / Q000379:methods; D013845:Thienamycins / Q000008:administration & dosage* / Q000737:chemistry* / Q000378:metabolism; D047392:beta-Cyclodextrins / Q000008:administration & dosage* / Q000737:chemistry* / Q000378:metabolism
chemical_list: D046911:Macromolecular Substances; D013845:Thienamycins; D047392:beta-Cyclodextrins; D000077731:Meropenem; C031215:betadex
keywords: Inclusion complex; Meropenem; Microbiological activity; Solubility; Stability; β-Cyclodextrin