Mucoadhesive nanoparticle composition comprising immunosuppresant and methods of use thereof

Abstract

Disclosed is a mucoadhesive nanoparticle delivery system for delivering an immunosuppressant, such as cyclosporine A, to a mucosal site for treatment of a disease or condition involving inflammation or excess immune activity. The system comprises nanoparticles formed from a plurality of linear amphiphilic block copolymers, each having a hydrophobic block comprising polylactide (PLA) and a hydrophilic block comprising dextran. The nanoparticles are surface-functionalized with a mucosal targeting moiety, such as a phenylboronic acid derivative, for targeted delivery and enhanced retention at the mucosal site. Pharmaceutical compositions, methods, and uses thereof comprising the mucoadhesive nanoparticle delivery system are disclosed. The compositions can be administered in an effective amount for treating the disease or condition while substantially preserving or restoring the function and/or integrity of the mucosal lining. The composition may be formulated as an aqueous suspension for administration to an anterior surface of the eye in the treatment of dry eye syndrome.