DEVELOPMENT OF TRIAMCINOLONE ACETONIDE NANOCRYSTALS FOR OCULAR ADMINISTRATION

AWDE ALFONSO, HAMOUDI G.; MARÍA LINA FORMICA; ALEJANDRO JAVIER PAREDES; LUIS IGNACIO TÁRTARA

Congreso; Annual Meeting of Bioscience Societies 2021; 2021

Objectives: Triamcinolone acetonide (TA) is a powerful anti-inflammatory drug, used in the treatment of inflammatory ocular disorders.Poor drug solubility and ocular anatomical barriers hinder an optimum therapy. The principal problems related to the use of injectableapproved formulations of TA include particle size (>1µm), which canhinder the administration, and also the presence of excipients aspreservatives, which can generate cell damage. The purpose of thiswork was to obtain a formulation based on triamcinolone acetonidenanocrystals (TA-NCs) to improve ocular corticosteroid therapy.Material and Methods: The microsphere assisted nanomilling(MAN) followed by spray-drying (SPA) techniques were used to obtain dried TA-NCs, which were characterized by studies of dynamic light scattering (DLS), Fourier-transform infrared spectroscopy(FTIR), thermal analysis, X-ray diffraction (XRD), and Electron microscopy (SEM). Preliminary studies of anti-inflammatory efficacy ofa suspension of dispersable TA-NCs via subconjunctival route (n=5)were carried out in an endotoxin-induced uveitis (EIU) rabbit modeland compared with a control group (normal saline solution).Results: Dispersable TA-NCs presented an average particle size of(266±77) nm; a narrow size distribution and zeta potential of (-27±1)mV, which remained stable during 30 days under storage conditionsat 4 °C. TA-NCs showed uniform and spherical morphology (SEM).FTIR and XRD spectra showed no apparent chemical and crystallinity changes, while no apparent thermal changes were revealed bythermal analysis. The subconjunctival administration of TA-NCs in albino male white rabbits did not show clinical signs of ocular damage. In vivo preliminary studies showed that dispersable TA-NCstreatment alleviated the inflammatory response in the anterior chamber and iris in EUI rabbit eyes.Conclusion: Dispersable TA-NCs are a promising approach to obtain a novel nanometric TA formulation for ocular disorders.