INJECTABLE SUSTAINED RELEASE COMPOSITION AND METHOD OF USING THE SAME FOR TREATING INFLAMMATION IN JOINTS AND PAIN ASSOCIATED THEREWITH
Described herein are injectable corticosteroid-loaded microparticles, pharmaceutical composition thereof and methods for reducing inflammation or pain in a body compartment such as a joint, an epidural space, a vitreous body of an eye, a surgically created space, or a space adjacent to an implant.
1 . A method for treating inflammation or pain in a patient in need thereof, the method comprising administering to the patient an extended release formulation, wherein the extended release formulation comprises a plurality of microparticles having core/shell morphology, wherein the microparticle includes (1) a crystalline drug core of more than 70% by weight of the microparticle, wherein the crystalline drug core includes one or more crystals of a corticosteroid, a salt or ester thereof; and (2) a polymeric shell encapsulating the crystalline drug core, whereby the polymeric shell is in contact but immiscible with the crystalline drug core.
2 . The method according to claim 1 , wherein the inflammation or pain is due to at least one of osteoarthritis, rheumatoid arthritis or injury induced arthritis, spinal disc protrusion, spinal nerve inflammation in cervical, thoracic or lumbar, chronic low back pain from nerve root compression, diabetic macular edema or uveitis, recurrent capsular contractions or keloid scarring.
3 . The method according to claim 1 wherein administering the extended release formulation comprises locally injecting to an affected joint, an epidural space, vitreous body, an epidural space, or a space adjacent to an implant having scar tissue of said patient.
4 . The method according to claim 3 wherein the corticosteroid is released locally within the body compartment and provides below a quantifiable limit of plasma corticosteroid 7 days after injection.
5 . The method according to claim 1 , wherein the corticosteroid is selected from fluticasone, fluticasone furoate, and fluticasone propionate.
6 . The method according to claim 1 , wherein the polymeric shell comprises one or more of the polymers selected from the group consisting of polyvinyl alcohol (PVA), poly(p-xylylene) polymers (trademarked as Parylene®), poly(lactic acid) (PLA), poly(glycolic acid) (PGA), poly(lactic-co-glycolic acid) (PLGA), poly(ε-caprolactone) (PCL), poly(valerolactone) (PVL), poly(ε-decalactone) (PDL), poly(1,4-dioxane-2,3-dione), poly(1,3-dioxane-2-one), poly(para-dioxanone) (PDS), poly(hydroxybutyric acid) (PHB), poly(hydroxyvaleric acid) (PHV), ethylene vinyl acetate (EVA) and poly(β-malic acid) (PMLA).
7 . The method according to claim 6 , wherein the polymeric shell comprises one or more of the polymers selected from the group consisting of polyvinyl alcohol (PVA), poly(p-xylylene) polymers (trademarked as Parylene®), poly(lactic acid) (PLA), poly(glycolic acid) (PGA), poly(lactic-co-glycolic acid) (PLGA), poly(ε-caprolactone) (PCL), poly(valerolactone) (PVL), poly(ε-decalactone) (PDL), poly(1,4-dioxane-2,3-dione), poly(1,3-dioxane-2-one), poly(para-dioxanone) (PDS), poly(hydroxybutyric acid) (PHB), poly(hydroxyvaleric acid) (PHV), ethylene vinyl acetate (EVA) and poly(β-malic acid) (PMLA).
8 . The method according to claim 5 , wherein said microparticles have a mean diameter of between 50 μm and 400 μm.
9 . The pharmaceutical composition according to claim 8 , wherein said microparticles have a mean diameter of between 80 μm and 150 μm.