Chitosan and Anionic Solubility Enhancer Sulfobutylether-β-Cyclodextrin-Based Nanoparticles as Dexamethasone Ophthalmic Delivery System for Anti-Inflammatory Therapy

Abstract

Cataract surgery interventions are constantly increasing, particularly among adult and elderly patients. This type of surgery can lead to inflammatory states of the ocular anterior segment (AS), usually healed via postoperative treatment with dexamethasone (DEX)-containing eye drops. The application of eye drops is challenging due to the high number of daily administrations. In this study, mucoadhesive nanoparticles (NPs) were formulated to improve the residence time of DEX on the corneal mucosa, enhancing the drug’s solubility and bioavailability. The NPs were generated using an ionotropic gelation technique, exploiting the interaction between the cationic group of chitosan (CS) and the anionic group of sulfobutylether-β-cyclodextrin (SBE-β-CD). The formation of the inclusion complex and its stoichiometry were studied through phase solubility studies, Job’s plot method, and Bi-directional transport studies on MDCKII-MDR1. The obtained NPs showed good chemical and physical characteristics suitable for drug loading and subsequent testing on animal mucosa. The DEX-loaded CS/SBE-β-CD NPs exhibited a prolonged residence time on animal mucosa and demonstrated enhanced drug permeability through the corneal membrane, showing a sustained release profile. The developed NPs posed no irritation or toxicity concerns upon local administration, making them an optimal and innovative drug delivery system for inflammatory AS diseases treatment.

Mucoadhesive Budesonide Solution for the Treatment of Pediatric Eosinophilic Esophagitis

“…A higher J leads to an increase in drug permeation, resulting in a higher BU concentration in the treated area. This peculiarity gives an evident advantage, especially in the case of the local treatment of pathological conditions of the esophageal mucosa, where the low residence time of the formulation limits the accumulation of the drug and thus the effectiveness of the treatment [51]. This evidence led us to select B1 as the most promising vehicle to deliver BU for the treatment of EoE, thanks to the enhanced water solubility and mucoadhesive properties.…”

“…To determine the mucoadhesive properties of the tested formulations, in vitro mucoadhesive studies were performed on freshly excised bovine esophagus with a slightly modified wash-off method [51]. The three formulations (F1, F2, and F3) loaded with 1 mg/mL of fluorescein diacetate (FD) were tested.…”