Key words: moxifloxacin, 2-hydroxypropyl-β-cyclodextrin (HPCD), «guest—host» inclusion complex, supercritical fluids (SCF), Rapid Expansion of Supercritical Solutions (RESS), FTIR spectroscopy, drug release kinetics
A new method to synthesize «guest—host» inclusion complex of moxifloxacin (MF)
with 2-hydroxypropyl-β-cyclodextrin (HPCD) based on the supercritical fluid
technologies in RESS (Rapid Expansion of Supercritical Solutions) regime was
suggested for further development of new drug formulations with improved
bioavailability. Using the RESS method, the MF-HPCD complex was obtained as 2—4
micron particles, which are optimal for both oral and inhalation forms of the drug
based on MF. According to the scanning electron microscopy data, the morphology of
MF-HPCD particles obtained via RESS processing is different from both initial
components and from MF-HPCD complex obtained by lyophilization from aqueous
solution. According to the X-ray diffraction data, the crystallinity of MF drops from 95
to 20—30% upon the formation of the complex with HPCD. The IR spectroscopic and
equilibrium dialysis data demonstrated that RESS provides higher efficiency of the
drug substance inclusion in the complex with HPCD compared to traditional methods
such as lyophilization or solid-phase components mixing.
doi:10.1134/S1990793118070126