Spray dried nanospheres for inclusion complexes of cefpodoxime proxetil with β-cyclodextrin,...

The aim of the current research was the development hard cellulose capsules containing cefpodoxime proxetil (CEF) (BCS-Class II) encapsulated nanospheres of inclusion complexes with β-CD, HP-β-CD and M-β-CD for efficient antibacterial therapy.

The reason for this phenomenon is to bring an innovative approach to effective oral antimicrobial therapy with hard cellulose capsules containing spray dried nanospheres of CEF with β-CD, HP-β-CD and M-β-CD by means of increased solubility, dissolution rate and improved antibacterial efficiency with lower oral dose.

Phase solubility analyses was performed to evaluate the drug/CD interaction, involving the stoichiometry and apparent stability constant. Following the preparation of inclusion complexes by spray-drying method, complexes were characterized for physical, solid-state and microbiological analyses. In vitro dissolution from hard cellulose capsules containing CEF and CEF/β-CD, CEF/HP-β-CD and CEF/M-β-CD complexes were performed.

According to A_L type phase solubility curves, complexes were formulated as 1:1 molar ratio. The solubility of pure CEF was determined as 0.241 ± 0.002 mg mL^-1, the solubility of inclusion complexes increased solubility from 3 to 5 times. The strong host-guest interaction was confirmed for CEF/HP-β-CD and CEF/M-β-CD complexes with SEM, DSC, FT-IR and ¹H-NMR analyses. Inclusion complexes were more efficient on bacterial cells (2-4 fold) than pure CEF both Staphylococcus aureus, Escherichia coli and Klebsiella pneumoniae. Hard-cellulose capsules filled with inclusion complexes exhibited significantly faster release than unprocessed CEF.

Hard-cellulose capsules containing CEF/HP-β-CD and CEF/M-β-CD complexes appear to be superior alternative to commercially available CEF tablets for effective antibacterial therapy.