Development and characterization of lyophilized cefpodoxime proxetil-Pluronic(R) F127/polyvinylpyrrolidone K30 solid dispersions with improved dissolution and enhanced antibacterial activity


PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, vol.26, no.4, pp.476-489, 2021 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 26 Issue: 4
  • Publication Date: 2021
  • Doi Number: 10.1080/10837450.2021.1889584
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Business Source Elite, Business Source Premier, Chemical Abstracts Core, EMBASE, International Pharmaceutical Abstracts, MEDLINE
  • Page Numbers: pp.476-489
  • Keywords: Cefpodoxime proxetil, Pluronic(&#174), F127, polyvinylpyrrolidone, solid dispersion, dissolution rate, antibacterial activity
  • Anadolu University Affiliated: Yes


The aim of this study was the development of hard-cellulose capsules containing cefpodoxime proxetil (CEF) (BCS Class II) loaded novel Pluronic(R) F127 (P127)/Polyvinylpyrrolidone K30 (PVP) solid dispersions (SDs) using ultrasonic probe induced solvent-lyophilization method for effective antibacterial treatment by means of improved saturated aqueous solubility, dissolution rate, reduced particle size, and wettability. SDs were evaluated for physical and solid-state analyses. The solubility of pure CEF was calculated as 0.269 +/- 0.005 mg/mL, SDs formulated with P127/PVP exhibited increased solubility from 3.5- to 8-fold. Molecular distribution of CEF in SDs and formation of CEF loaded amorphous polymeric network were confirmed with morphological study, thermal analysis, Fourier-transform infrared spectroscopy (FT-IR), and H-1-NMR studies. Staphylococcus aureus (ATCC 29213), Escherichia coli (ATCC 25922), and Klebsiella pneumoniae (ATCC 700603) were used to investigate the antibacterial effectiveness of the SDs. The minimum inhibitory concentration (MIC) values of the P127/PVP SDs were found 2-8 times lower than the pure CEF. All SDs from hard-cellulose capsules exhibited significantly faster release than unprocessed CEF. The profiles of SDs and reference were detected to be dissimilar according to difference (f(1)) and similarity factor (f(2)). Hard-cellulose capsules containing CEF loaded P127/PVP SDs appear to be feasible alternative to commercially available CEF tablets for effective antibacterial therapy at lowest dose.