Development of Triamcinolone Acetonide Nanocrystals for Ocular Administration

Abstract

Triamcinolone acetonide (TA) is a powerful anti-inflammatory drug used in the treatment of inflammatory ocular disorders; however, its poor aqueous solubility and ocular anatomical barriers hinder optimal treatment. The aim of this work was to obtain triamcinolone acetonide nanocrystals (TA-NC) to improve ocular corticosteroid therapy. Self-dispersible TA-NC were prepared by the bead milling technique followed by spray-drying, exhaustively characterized and then evaluated in vivo in an ocular model of endotoxin-induced uveitis (EIU). Self-dispersible TA-NC presented an average particle size of 257 ± 30 nm, a narrow size distribution and a zeta potential of −25 ± 3 mV, which remained unchanged for 120 days under storage conditions at 25 °C. In addition, SEM studies of the TA-NC showed uniform and spherical morphology, and FTIR and XRDP analyses indicated no apparent chemical and crystallinity changes. The subconjunctival administration of TA-NC in albino male white rabbits showed no clinical signs of ocular damage. In vivo studies proved that treatment with self-dispersible TA-NC alleviated the inflammatory response in the anterior chamber and iris in EUI rabbit eyes. Dispersible TA-NC are a promising approach to obtaining a novel nanometric TA formulation for ocular disorders.

Design and Development of Sublingual Printlets Containing Domperidone Nanocrystals Using 3D Melting Solidification Printing Process (MESO-PP)

“…Taking into account the limitations associated with the low solubility of some drugs, our group has worked extensively to obtain nanocrystals (NCs) by a “top-down” method, successfully achieving the nanometrization of different active pharmaceutical ingredients (API) [ 12 , 13 , 14 ]. NCs are solid particles of a drug with crystalline characteristics and sizes in the nanometric range, typically between 200 and 500 nm [ 15 ]. NCs are surrounded by a layer of stabilizer to prevent aggregation and can be prepared either as suspensions—commonly named nanosuspensions—or as powder, which is obtained by removing the solvent from the nanosuspension.…”

Nanoparticles in Ocular Drug Delivery Systems

“…We are delighted to present the latest research and review works reporting on the use of nanoparticles and other nanosystems in ophthalmic formulations to increase the bioavailability of drugs, improving their therapeutic efficacy. The articles selected for this Special Issue are the following: “Development of Triamcinolone Acetonide Nanocrystals for Ocular Administration” [ 1 ]. “Design, Characterization and Pharmacokinetic–Pharmacodynamic Evaluation of Poloxamer and Kappa-Carrageenan-Based Dual-Responsive In Situ Gel of Nebivolol for Treatment of Open-Angle Glaucoma” [ 2 ].…”