Mucoadhesive brinzolamide-loaded nanofibers for alternative glaucoma treatment

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 180; pp. 48 - 62
• Main Authors: Cegielska, Olga, Sierakowski, Maciej, Sajkiewicz, Paweł, Lorenz, Kairi, Kogermann, Karin
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.11.2022
• Subjects: Cyclodextrins; Drug delivery system; Electrospinning; Glaucoma; Mucoadhesion; Nanofibers; Topical administration; Glaucoma; Electrospinning; Cyclodextrins; Nanofibers; Mucoadhesion; Drug delivery system; Topical administration
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2022.09.008

[Display omitted] Despite the advances in the field of pharmaceutical materials and technology, topical administration remains a method of choice for the treatment of eye diseases such as glaucoma, with eye drops being a leading dosage form. Their main disadvantage is a very short drug residence time and thus poor drug bioavailability, leading to the necessity of continuous repeated dosing. Mucoadhesive electrospun nanofibers are promising candidates for overcoming these challenges, while still benefiting from topical ocular administration. As an alternative for eye drops, a nanofibrous drug delivery system (DDS) for the delivery of brinzolamide (BRZ), based on β-cyclodextrin (β-CD), hydroxypropyl cellulose (HPC) and polycaprolactone (PCL), was designed. The results showed β-CD/BRZ guest–host interactions, successful drug incorporation into the nanofibers, and the possibility of more accurate dosing in comparison with the control eye drops. Drug permeation through sheep corneas was almost linear in time, achieving therapeutic concentrations in the receptor medium, and mucoadhesion to sheep eye mucosa was relatively high in case of formulations with high HPC content. All formulations were biocompatible, their mechanical properties were sufficient to handle them without caution and UV irradiation was suitable to reduce bioburden of the fibers matrix, yet no antibacterial properties of BRZ were observed.