Binary and ternary complexes of norfloxacin with hydroxypropyl ß cyclodextrin and amino acids to improve the solubility of the pharmaceutical active ingredient

PONCE PONTE MICAELA; CAROLINA ALOISIO; ROMERO GUERRA DIANA MARCELA; GRACIA-VAZQUEZ SANDRA; CLAUDIA GARNERO; MARCELA LONGHI

Therapeutic Delivery

Future Science Ltd

Lugar: London; Año: 2019 vol. 9 p. 639 - 652

2041-5990

Aim: Binary and ternary complexes with hydroxypropyl-β-cyclodextrin (HPβCD), using glutamic acid (GA),proline or lysine as the third component, were developed to increase the solubility and the dissolutionrate of norfloxacin (NOR). Methods/results: Complexation was evaluated by phase solubility studies, obtaining the highest NOR solubility with GA and HPβCD. Thermal analysis suggested that different kindsof interactions occur among NOR, HPβCD and each amino acid, and when the systems were prepared bykneading or by means of freeze-drying technique. Dissolution studies, performed on simulated gastricfluid and subsequent simulated intestinal fluid, showed the highest rate of NOR from NOR?HPβCD?GA.Conclusion: NOR:HPβCD:GA was the best approach for improving the bioavailability of NOR.