Inclusion complexes of the steroid hormones 17β-estradiol and progesterone with β- and γ-cyclodextrin hosts: syntheses, X-ray structures, thermal analyses and API solubility enhancements

• Alexios I. Vicatos,
• Zakiena Hoossen and
• Mino R. Caira

Beilstein J. Org. Chem. 2022, 18, 1749–1762, doi:10.3762/bjoc.18.184

• . Furthermore, no previous structure determinations via SCXRD analysis of CD complexes of BES and PRO have been reported. Many studies involved phase solubility analyses to determine CD complex formation and association constants. Our previous study of the complexation of the steroidal anticancer agent 2

• -methoxyestradiol (2ME) by selected CDs [39] yielded two significant positive outcomes, namely a considerable increase in the aqueous solubility and dissolution rate of 2ME derived from its β-CD complex, and for the first time, the determination of the modes of inclusion of a steroidal molecule within the cavities

Inclusion complexes of 2-methoxyestradiol with dimethylated and permethylated β-cyclodextrins: models for cyclodextrin–steroid interaction

• Mino R. Caira,
• Susan A. Bourne,
• Halima Samsodien and
• Vincent J. Smith

Beilstein J. Org. Chem. 2015, 11, 2616–2630, doi:10.3762/bjoc.11.281

• Mino R. Caira Susan A. Bourne Halima Samsodien Vincent J. Smith Centre for Supramolecular Chemistry Research (CSCR), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa 10.3762/bjoc.11.281 Abstract The interaction between the potent anticancer agent 2-methoxyestradiol

• -methoxyestradiol; solubility; X-ray diffraction; Introduction This report focuses on the modes of inclusion of the anticancer agent 2-methoxyestradiol (2ME, Figure 1) in the host cyclodextrins (CDs) heptakis(2,6-di-O-methyl)-β-CD (DIMEB) and heptakis(2,3,6-tri-O-methyl)-β-CD (TRIMEB) in the solid state. The

• ongoing clinical trials with 2ME continue to appear [6][7], attention has shifted towards its more promising derivatives, such as 2-methoxyestradiol-3,17-di,O-bis-sulfamate (2MES), with higher potency and improved pharmacokinetic properties [8]. Nevertheless, as noted in our recent report on some aspects