US2023058971A1PendingUtilityA1

Extended release microparticles and suspensions thereof for medical therapy

69
Assignee: GRAYBUG VISION INCPriority: May 10, 2017Filed: Nov 18, 2021Published: Feb 23, 2023
Est. expiryMay 10, 2037(~10.8 yrs left)· nominal 20-yr term from priority
Inventors:Ming YangJeffrey L. ClelandYun YuWeiling YuJoshua Kays
A61K 31/216A61K 31/404A61K 9/5031A61K 31/5377A61K 31/542A61K 31/498A61K 9/0051A61K 31/122A61K 47/54A61K 31/4155A61P 27/02A61K 31/382
69
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Claims

Abstract

An improved microparticle or lyophilized or otherwise reconstitutable microparticle composition thereof for medical therapy, including ocular therapy.

Claims

exact text as granted — not AI-modified
We claim: 
     
         1 . A method for the treatment of an ocular disorder selected from glaucoma, wet-age related macular degeneration, dry-age related macular degeneration, or a disorder related to an increase in intraocular pressure comprising suprachoroidal administration of an effective amount of solid aggregating biodegradable microparticles optionally in a pharmaceutically acceptable carrier wherein the solid aggregating biodegradable microparticles comprise a prodrug of a therapeutically active compound encapsulated in (a) poly(lactic-co-glycolic acid) (PLGA) and/or polylactic acid (PLA) and (b) poly(lactic-co-glycolic acid) conjugated to polyethylene glycol (PLGA-PEG), and a surfactant, wherein the microparticles:
 (i) have a mean diameter between 10 μm and 60 μm;   (ii) have been surface-modified with a surface treatment agent to partially degrade surface polymer at a temperature less than about 18° C. wherein the surface treatment agent comprises an aqueous base and an organic solvent;   (iii) aggregate in vivo to form at least one larger pellet in vivo that provides sustained drug delivery in vivo for at least three months; and   (iv) wherein the prodrug is selected from the formula:   
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof 
       wherein 
       x and y are independently selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10; and 
       x′ and y′ are independently selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10. 
     
     
         2 . The method of  claim 1 , wherein x and y are independently selected from 1, 2, 3, 4, 5, and 6. 
     
     
         3 . The method of  claim 1 , wherein x′ and y′ are independently selected from 1, 2, 3, 4, 5, and 6. 
     
     
         4 . The method of  claim 1 , wherein y is 2, 3, or 4 and y′ is 2, 3, or 4. 
     
     
         5 . The method of  claim 1 , wherein the prodrug is of the formula 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         6 . The method of  claim 5 , wherein y is 2, 3, or 4 and y′ is 2, 3, or 4. 
     
     
         7 . The method of  claim 6 , wherein the prodrug is of the formula 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         8 . The method of  claim 6 , wherein the prodrug is of the formula 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         9 . The method of  claim 1 , wherein at least one pellet provides sustained drug delivery for at least 4 months. 
     
     
         10 . The method of  claim 1 , wherein at least one pellet provides sustained drug delivery for at least 5 months. 
     
     
         11 . The method of  claim 1 , wherein at least one pellet provides sustained drug delivery for at least 6 months. 
     
     
         12 . The method of  claim 1 , wherein the solid aggregating biodegradable microparticles have a mean diameter between about 20 and 50 μm. 
     
     
         13 . The method of  claim 1 , wherein the solid aggregating biodegradable microparticles have a mean diameter between about 20 and 40 μm. 
     
     
         14 . The method of  claim 1 , wherein the solid aggregating biodegradable microparticles have a mean diameter between about 20 and 30 μm. 
     
     
         15 . The method of  claim 1 , wherein the solid aggregating biodegradable microparticles have a mean diameter between about 25 and 40 μm. 
     
     
         16 . The method of  claim 1 , wherein the solid aggregating biodegradable microparticles have a mean diameter between about 25 and 35 μm. 
     
     
         17 . The method of  claim 1 , wherein the aqueous base is a hydroxide base. 
     
     
         18 . The method of  claim 1 , wherein the aqueous base is sodium hydroxide. 
     
     
         19 . The method of  claim 1 , wherein the aqueous base is potassium hydroxide. 
     
     
         20 . The method of  claim 17 , wherein the organic solvent is an alcohol. 
     
     
         21 . The method of  claim 20 , wherein the alcohol is ethanol. 
     
     
         22 . The method of  claim 20 , wherein the alcohol is methanol. 
     
     
         23 . The method of  claim 21 , wherein the surface treatment agent comprises ethanol and sodium hydroxide. 
     
     
         24 . The method of  claim 1 , wherein the surface has been modified at a temperature not more than 16° C. 
     
     
         25 . The method of  claim 1 , wherein the surface has been modified at a temperature not more than 10° C. 
     
     
         26 . The method of  claim 1 , wherein the surface has been modified at a temperature not more than 8° C. 
     
     
         27 . The method of  claim 1 , wherein the surface has been modified at a temperature not more than 5° C. 
     
     
         28 . The method of  claim 1  for the treatment of glaucoma. 
     
     
         29 . The method of  claim 1  for the treatment of wet-age related macular degeneration. 
     
     
         30 . The method of  claim 1  for the treatment of dry-age related macular degeneration. 
     
     
         31 . The method of  claim 1  for the treatment of a disorder related to an increase in intraocular pressure. 
     
     
         32 . The method of  claim 1  wherein the ocular disorder for treatment is in a human.

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