Cellulose Acetate Phthalate-Based pH-Responsive Cyclosporine A-Loaded Contact Lens for the Treatment of Dry Eye

Int J Mol Sci. 2023 Jan 25;24(3):2361. doi: 10.3390/ijms24032361.

Abstract

Cyclosporine A (CsA) as an eye drop is an effective treatment for dry eye. However, it has potential side effects and a short ocular residence time. To overcome these obstacles, we developed a cellulose acetate phthalate-based pH-responsive contact lens (CL) loaded with CsA (CsA-CL). The CsA was continuously released from the CsA-CL at physiological conditions (37 °C, pH 7.4) without an initial burst. CsA was well-contained in the selected storage condition (4 °C, pH 5.4) for as long as 90 days. In safety assays, cytotoxicity, ocular irritation, visible light transmittance, and oxygen permeability were in a normal range. CsA concentrations in the conjunctiva, cornea, and lens increased over time until 12 h. When comparing the therapeutic efficacy between the normal control, experimental dry eye (EDE), and treatment groups (CsA eye drop, naïve CL, and CsA-CL groups), the tear volume, TBUT, corneal fluorescein staining at 7 and 14 days, conjunctival goblet cell density, and corneal apoptotic cell counts at 14 days improved in all treatment groups compared to EDE, with a significantly better result in the CsA-CL group compared with other groups (all p < 0.05). The CsA-CL could be an effective, stable, and safe option for inflammatory dry eye.

Keywords: contact lens; cyclosporine A; dry eye; supercritical fluid technique.

MeSH terms

  • Contact Lenses*
  • Cyclosporine / therapeutic use
  • Dry Eye Syndromes* / drug therapy
  • Humans
  • Hydrogen-Ion Concentration
  • Ophthalmic Solutions / therapeutic use
  • Tears

Substances

  • Cyclosporine
  • cellulose acetate phthalate
  • Ophthalmic Solutions

Grants and funding

This research received no external funding.