Taste-masking and colloidal-stable cubosomes loaded with Cefpodoxime proxetil for pediatric oral delivery

Int J Pharm. 2020 Feb 15:575:118875. doi: 10.1016/j.ijpharm.2019.118875. Epub 2019 Nov 22.

Abstract

Drug administration failure has been often witnessed in pediatric due to children's resistance to take medicines with bitter taste. Taste-masking is the key requirement among the scanty drugs available for children. Solid taste-masking systems, such as tablets and capsules, are difficult to swallow for children. Therefore, a liquid taste-masking system based on lyotropic liquid crystalline nanoparticles (LLCNs) was developed in this study. Cefpodoxime proxetil (CFP), a typically bitter drug used as antibiotic in pediatric, was selected as the model drug, and the encapsulation of CFP into the LLCNs was envisaged to improve their taste. Pluronic F127 was added to improve the colloidal stability of CFP-LLCNs. The optimized CFP-LLCNs showed the particle size of 187.29 ± 4.12 nm and the encapsulation efficiency of 85.80%. The mesophase analysis by polarized light microscopy and small angle X-ray scattering confirmed the cubic phase of CFP-LLCNs. It showed a sustained-release profile well fitted to Higuchi model, indicating that diffusion and erosion were both responsible for the CFP release. The taste-masking ability of CFP-LLCNs was confirmed by electronic tongue, compared to CFP and commercial product. The colloidal stability was verified after 3 months storage in room condition (25 ± 2 °C, 70 ± 2%RH). To sum up, the taste-masking and colloidal-stable CFP-LLCNs showed great potential for pediatric oral delivery.

Keywords: Cefpodoxime proxetil; Lyotropic liquid crystal; Pediatric oral delivery; Taste-masking.

MeSH terms

  • Administration, Oral
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / chemistry
  • Cefpodoxime Proxetil
  • Ceftizoxime / administration & dosage
  • Ceftizoxime / analogs & derivatives*
  • Ceftizoxime / chemistry
  • Child
  • Colloids
  • Drug Delivery Systems*
  • Drug Liberation
  • Drug Stability
  • Electronic Nose
  • Gastric Juice / chemistry
  • Humans
  • Intestinal Secretions / chemistry
  • Liquid Crystals*
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Taste*

Substances

  • Anti-Bacterial Agents
  • Colloids
  • Ceftizoxime