The Bioadhesive-Thermoresponsive Ophthalmic Gel Loaded Solid Dispersion of Triamcinolone Acetonide For Improvement of Ocular Inflammation Therapy 

Abstract

Background: In developed countries, 10% of blindness cases are caused by uveitis (UV). Triamcinolone acetonide (TA) is a corticosteroid that has been widely used for the treatment of ocular inflammation both in intravitreal injection preparations or as an eye drop. The solubility of TA which is practically insoluble in water is an obstacle to its development. Objectives: This study aims to improve the therapeutic effectiveness of ocular inflammation by increasing the solubility of Triamcinolone acetonide (TA) as a hydrophobic drug. The enhancement of solubility allows for better bioavailability so it can optimize the therapy of UV. Methods: The solid dispersion method was selected to enhance the solubility of TA by comparing solvent-evaporation and freeze-drying methods. The solid dispersion method (SD-TA) was made with PEG 6000 and PVP-K30 as surfactants and then characterized by FTIR, XR diffraction, and SEM. Furthermore, SD-TA was mixed into the gel base and an ex vivo study was for ensure the local therapy. Result: The solvent-evaporation method produced more soluble TA than the freeze-drying method. F9 dissolved TA was ten times higher than pure TA (p<0.05). The G4c gel formula showed the ability to retain TA 3.15±0.15 mg at 24 h. Neither the G4c gel formula nor the SD-TA formula (F9) showed hemolysis activity. The gel also exhibits isotonic characteristics and did not cause any structural destruction of the RBCs. Conclusion: This study successfully demonstrated the morphological and structural changes of TA in SD-TA which proved to increase TA solubility and potentially provide local therapeutic effects by bioadhesive-thermoresponsive gel for better treatment of inflammation in the eye such as uveitis.