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AssigneeUniversity of Waterloo
InventorsFrank Xiaofei GU, Shengyan LIU, Lyndon William James JONES
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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.
A method for treating a disease or condition involving inflammation, comprising topically administering a pharmaceutical composition to a mucosal surface of a subject, the composition comprising nanoparticles capable of releasing an immunosuppressant, the nanoparticles comprising a plurality of linear amphiphilic block copolymers including a hydrophilic block and a hydrophobic block, the hydrophobic block comprising polylactide (PLA) and the hydrophilic block comprising dextran (Dex), the nanoparticles being functionalized with a mucosal targeting moiety.
A method for hydrating a mucosal surface comprising topically administering to the mucosal surface a pharmaceutical composition comprising nanoparticles, the nanoparticles comprising a plurality of linear amphiphilic block copolymers each including a hydrophilic block and a hydrophobic block, the hydrophilic block comprising dextran (Dex) and the hydrophobic block comprising polylactide (PLA), the nanoparticles being functionalized with a mucosal targeting moiety.
A topical pharmaceutical composition for the treatment of dry eye syndrome, the composition being an aqueous suspension for administration to the anterior surface of the eye, the composition comprising nanoparticles capable of releasing cyclosporine A, the nanoparticles comprising a plurality of linear amphiphilic block copolymers including a hydrophilic block and a hydrophobic block, the hydrophobic block comprising polylactide (PLA) and the hydrophilic block comprising dextran (Dex), the nanoparticles being functionalized with a mucosal targeting moiety, wherein the concentration of cyclosporine A in the composition is about 0.001% to about 0.1% wt/vol, and wherein the composition is formulated for administration of cyclosporine A at an overall dose of less than about 150.0 μg per week and an administration frequency of less than 10 times per week.
Dependencies are inferred from the claim text.