Biopolymer-based nanoparticles with tunable mucoadhesivity efficiently deliver therapeutics across the corneal barrier

To overcome the natural barriers of the ocular system that limit the topical delivery of therapeutically active molecules to the posterior eye, nanoscale drug carriers can be used to improve transcorneal drug transport. So far, using mucoadhesive drug carriers has been put forward as the most promising strategy to optimize drug transport.

Highlights

Chitosan/alginate blends were electrosprayed to form drug carrier nanoparticles.

Polymeric nanoparticles showed good stability and a sustained drug release.

Moderate mucoadhesivity ensures optimal drug transport across the corneal barrier.

Mucoadhesion of nanoparticles can be adjusted regarding the particular application.

However, if the mucoadhesivity of a drug carrier is too high, this might limit the diffusive entry of molecules/drug carriers into the vitreous. In this study, we show how modulating the net charge of biopolymer-based drug carrier particles alters not only their mucoadhesivity but also other important properties, e.g., their stability, drug loading capacity and drug release profiles. Compared to simple aqueous solutions of free drug molecules as used in current treatments, nanoparticulate drug carriers with intermediate mucoadhesivity show improved drug transport across the corneal barrier.

Therefore, our study shows that mucoadhesion of drug carrier particles is a feature that needs to be considered with great care – not only for ocular delivery attempts but for all drug delivery approaches dealing with mucosal barriers.

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Article information: Ceren Kimna, Benjamin Winkeljann, Julia Hoffmeister, Oliver Lieleg. Materials Science and Engineering: C, Volume 121, 2021. https://doi.org/10.1016/j.msec.2021.111890.