US 12,109,302 B2
Sustained release biodegradable intracanalicular inserts comprising a hydrogel and cyclosporine
Charles D. Blizzard, Nashua, NH (US); Rami El-Hayek, Norwood, MA (US); Michael Goldstein, Cambridge, MA (US); Peter Jarrett, Burlington, MA (US); and Andrew Vanslette, Bolton, MA (US)
Assigned to Ocular Therapeutix, Inc., Bedford, MA (US)
Filed by Ocular Therapeutix, Inc., Bedford, MA (US)
Filed on Jul. 28, 2023, as Appl. No. 18/227,463.
Application 18/227,463 is a continuation of application No. 17/681,238, filed on Feb. 25, 2022, granted, now 11,779,536.
Application 17/681,238 is a continuation of application No. 17/483,220, filed on Sep. 23, 2021, granted, now 11,331,267, issued on May 17, 2022.
Claims priority of provisional application 63/124,204, filed on Dec. 11, 2020.
Claims priority of provisional application 63/082,505, filed on Sep. 24, 2020.
Prior Publication US 2024/0041758 A1, Feb. 8, 2024
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/00 (2006.01); A61K 38/13 (2006.01); A61K 47/10 (2017.01); A61K 47/22 (2006.01); A61P 27/02 (2006.01)
CPC A61K 9/0051 (2013.01) [A61K 38/13 (2013.01); A61K 47/10 (2013.01); A61K 47/22 (2013.01); A61P 27/02 (2018.01)] 20 Claims
 
1. A method of treating an ocular disease in a human subject in need thereof, the method comprising inserting into the canaliculus of the subject a sustained release biodegradable intracanalicular insert comprising a hydrogel and cyclosporine, wherein the cyclosporine is in the form of particles having d50 value of less than about 50 μm as measured by laser diffraction and wherein the cyclosporine particles are dispersed within the hydrogel, wherein the hydrogel comprises a polymer network comprising crosslinked polymer units that are identical or different which are polyethylene glycol units having two to ten arms, wherein the arms of the polyethylene glycol units are connected to a core molecule of pentaerythritol, the polymer network is formed by reacting an electrophilic group-containing multi-arm polymer precursor with a nucleophilic group-containing cross-linking agent, the electrophilic group is an N-hydroxysuccinimidyl (NHS) ester group, the nucleophilic group-containing crosslinking agent contains an amine group, wherein the ocular disease is selected from dry eye, blepharitis, allergic conjunctivitis, atopic keratoconjunctivitis or vernal keratoconjunctivitis.