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Cubogel as potential platform for glaucoma management.

Sinar Sayed1, Mostafa Abdel-Moteleb2, Maha Mohamed Amin1

  • 1Pharmaceutics and Industrial Pharmacy, Cairo University Faculty of Pharmacy, Cairo, Egypt.

Drug Delivery
|January 29, 2021
PubMed
Summary

This study developed a novel cubogel formulation to enhance the ocular delivery of Dorzolamide Hydrochloride (DZ), an antiglaucoma drug. The optimized cubogel significantly improved corneal permeability and bioavailability compared to existing eye drops.

Keywords:
CubogelIOPglaucomastability and corneal bioavailabilityterminal sterilization

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Ocular Therapeutics

Background:

  • Glaucoma is a leading cause of irreversible blindness worldwide.
  • Dorzolamide Hydrochloride (DZ) is a carbonic anhydrase inhibitor used to treat glaucoma.
  • Poor corneal permeability limits the efficacy of conventional ocular drug delivery systems for DZ.

Purpose of the Study:

  • To develop and characterize DZ-loaded cubogel as a potential ocular dosage form.
  • To enhance the transcorneal permeability and bioavailability of DZ.
  • To evaluate the safety and efficacy of the optimized cubogel formulation.

Main Methods:

  • Cubosomal dispersions loaded with DZ were prepared using Box-Behnken design.
  • Formulations were optimized based on particle size, zeta potential, and in vitro drug release.
  • The optimized cubogel was characterized using DSC, ex vivo permeation, stability studies, and in vivo assessments (Draize test, histology, CLSM, IOP measurement).

Main Results:

  • The optimized cubogel formulation exhibited favorable particle size (153.3 nm), zeta potential (-32 mV), and drug release (37.78% in 2h).
  • In vivo studies confirmed the safety and stability of the cubogel.
  • Confocal laser scanning microscopy (CLSM) demonstrated a 2.5-fold increase in corneal penetration.
  • The optimized cubogel achieved significantly higher bioavailability (288.24 mg·h/mL) compared to Trusopt® eye drops (115.40 mg·h/mL).

Conclusions:

  • DZ-loaded cubogel represents a promising ocular delivery system for enhancing transcorneal permeation.
  • This novel formulation offers improved corneal bioavailability of DZ for glaucoma treatment.
  • Cubogel technology holds potential for advancing ocular drug delivery strategies.