The Enhancement of Nasal Drug Absorption From Powder Formulations by the Addition of Sodium Carboxymethyl Cellulose

IEEE Trans Nanobioscience. 2016 Dec;15(8):798-803. doi: 10.1109/TNB.2016.2612682. Epub 2017 Jan 4.

Abstract

For nasal drug absorption, powder formulations can be expected to provide many advantages. The first aim of this study was to examine drug absorption following nasal administration of powder formulations in rats. Pharmaceutical excipients are typically added to most powder formulations. The second aim was to investigate the change in nasal drug absorption of powder formulations in the presence of sodium carboxymethyl cellulose (CMC-Na). Model drugs used were norfloxacin (NFX), warfarin (WF), and piroxicam (PXC). The absorption from bulk powders is different from that of solutions. The absorption of PXC and WF from powder formulations was enhanced compared to those of the other solutions, while that of NFX, which has a low solubility, was decreased, suggesting that the nasal absorption of many drugs, except poorly soluble drugs, is enhanced when they are administered as powder formulations. CMC-Na enhanced the absorption of NFX and PXC. The presence of CMC-Na slightly decreased the absorption of WF. In vitro transepithelial transport from the powder formulation was not affected by the presence of CMC-Na. Furthermore, the nasal retention of the powder formulation was significantly increased in the presence of CMC-Na. In conclusion, the nasal absorption of many drugs, except those that are poorly soluble, can be increased by administering them as a powder formulation and the nasal absorption of the formulation is enhanced further in the presence of CMC-Na.

MeSH terms

  • Absorption, Physiological / drug effects*
  • Administration, Intranasal
  • Animals
  • Carboxymethylcellulose Sodium / administration & dosage
  • Carboxymethylcellulose Sodium / chemistry
  • Carboxymethylcellulose Sodium / pharmacokinetics*
  • Carboxymethylcellulose Sodium / pharmacology*
  • Cell Membrane Permeability / drug effects
  • Chemistry, Pharmaceutical
  • Dogs
  • Madin Darby Canine Kidney Cells
  • Models, Chemical
  • Nasal Mucosa / chemistry
  • Nasal Mucosa / metabolism*
  • Norfloxacin / administration & dosage
  • Norfloxacin / blood
  • Norfloxacin / pharmacokinetics
  • Piroxicam / administration & dosage
  • Piroxicam / blood
  • Piroxicam / pharmacokinetics
  • Powders
  • Rats
  • Solubility
  • Warfarin / administration & dosage
  • Warfarin / blood
  • Warfarin / pharmacokinetics

Substances

  • Powders
  • Piroxicam
  • Warfarin
  • Carboxymethylcellulose Sodium
  • Norfloxacin