Phosphorylated xanthan gum-Ag(I) complex as antibacterial viscosity enhancer for eye drops formulation

Carbohydr Polym. 2021 Sep 1:267:118196. doi: 10.1016/j.carbpol.2021.118196. Epub 2021 May 14.

Abstract

Topical instillation of eye drops represents the treatment of choice for many ocular diseases. Ophthalmic formulations must meet general requirements, i.e. pH, osmolality, transparency and viscosity to ensure adequate retention without inducing irritation and the development of eye infections. We developed a phosphorylated xanthan gum-Ag(I) complex (XGP-Ag) showing pH (pH = 7.1 ± 0.3) and osmolality values (311 ± 2 mOsm/kg) close to that of human tears (pH = 6.5-7.6 and 304 ± 23 mOsm/kg) thanks to the presence of phosphate moieties along the chain. The presence of phosphate groups covalently bound to the XG chains avoids their dispersion in fluid, thus reducing the risk of corneal calcification. 0.02% w/v XGP-Ag solution showed high transparency (higher than 95% along the entire visible range), adequate refractive index (1.334 ± 0.001) and viscosity in the range: γ 1 s-1-10,000 s- 1 (26.4 ± 0.8-2.1 ± 0.4 mPa·s). Its cytotoxicity and capability to hinder bacterial proliferation was also verified.

Keywords: Antibacterial; Eye drops; Silver ions; Viscosity; Xanthan gum.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / toxicity
  • Coordination Complexes / chemistry
  • Coordination Complexes / pharmacology*
  • Coordination Complexes / toxicity
  • Humans
  • Mice
  • Microbial Sensitivity Tests
  • NIH 3T3 Cells
  • Ophthalmic Solutions / chemistry
  • Ophthalmic Solutions / pharmacology*
  • Ophthalmic Solutions / toxicity
  • Organophosphates / chemistry
  • Organophosphates / pharmacology
  • Organophosphates / toxicity
  • Phosphorylation
  • Polymers / chemistry
  • Polymers / pharmacology
  • Polymers / toxicity
  • Polysaccharides, Bacterial / chemistry
  • Polysaccharides, Bacterial / pharmacology*
  • Polysaccharides, Bacterial / toxicity
  • Pseudomonas fluorescens / drug effects
  • Refractometry
  • Rheology
  • Silver / chemistry
  • Silver / pharmacology*
  • Silver / toxicity
  • Staphylococcus epidermidis / drug effects
  • Viscosity / drug effects*

Substances

  • Anti-Bacterial Agents
  • Coordination Complexes
  • Ophthalmic Solutions
  • Organophosphates
  • Polymers
  • Polysaccharides, Bacterial
  • Silver
  • polyquaternium 1
  • xanthan gum