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US 2024/0197637 A1Published application
Polymeric microparticles for the local treatment of chronic inflammatory diseases
AssigneesFondazione Istituto Italiano Di Tecnologia, The University of North Carolina at Chapel Hill
InventorsPaolo DECUZZI, Martina DI FRANCESCO, Lara LONGOBARDI, Huseyin OZKAN
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Abstract
The present invention relates to drug-delivery compositions comprising microparticles with the shape of a prism comprising at least one polymer and at least one CCR2 inhibitor. Preferably said composition is for the treatment of local chronic inflammation diseases, such as osteoarthritis.
Claims20
1:
- A drug-delivery composition comprising one or more microparticles, wherein each microparticle has a shape of a prism with three or more sides, and each side has a side length comprised between about 5 and about 50 μm and a height length comprised between about 5 and about 50 μm, said microparticle comprising at least one polymer and at least one inhibitor of C-C Chemokine Receptor-2 (CCR2).
2:
- The drug-delivery composition according to claim 1 wherein said microparticle has the shape of a prism with a square base.
3:
- The drug-delivery composition according to claim 2 wherein the side length is of about 20 μm and the height length is of about 10 μm.
4:
- The drug-delivery composition of claim 1, wherein said microparticle has a Young's modulus under compression comprised between 1 KPa and 10 MPa, preferably from 100 KPa to 10 MPa.
5:
- The drug-delivery composition of claim 1, wherein said polymer is selected from the group consisting of poly(lactic-co-glycolic acid)(PLGA), polyethylene glycol (PEG), polycaprolactone (PCL), hyaluronic acid (HA), chitosan, gelatin and a combination thereof.
6:
- The drug-delivery composition of claim 1, wherein said CCR2 inhibitor is selected from the group consisting of RS504393, Maraviroc, cenicriviroc, CD192, CCX872, CCX140, 2-((Isopropylaminocarbonyl)amino)-N-(2-((cis-2-((4(methylthio)benzoyl)amino)cyclohexyl)amino)-2-oxoethyl)-5-(trifluoromethyl)-benzamide, vicriviroc, SCH351125, TAK779 and CCR2 antagonist 4.
7:
- The drug-delivery composition of claim 1, wherein said CCR2 inhibitor is loaded on a nanoparticle.
8:
- The drug-delivery composition of claim 1, wherein each microparticle comprises poly(lactic-co-glycolic acid)(PLGA) and RS504393.
9:
- The drug-delivery composition of claim 1, wherein said microparticle further comprises an anti-inflammatory drug, or dexamethasone.
10:
- The drug-delivery composition of claim 1, wherein said microparticle further comprises a drug selected from the group consisting of:
- glucocorticoids;
- non-steroidal anti-inflammatory drugs;
- monoclonal antibody against the tumor necrosis factor-alpha (TNF-α), certolizumab pegol;
- TNF-α inhibitors, Golimumab;
- antiplatelet drugs, Tirofiban;
- kinase inhibitors, such as Ruxolitinib;
- CLK/DYRK1A inhibitors, Lorecivivint;
- and Fetuin A.
6 more elements
11:
- The drug-delivery composition of claim 1, wherein said microparticle further comprises one or more nanoparticles, lipidic and polymeric nanoparticles or short interfering RNA (siRNA)-loaded nanoparticles.
12:
- The drug-delivery composition of claim 1, for use as a medicament.
13:
- A method for treating or preventing a localized chronic inflammation disease comprising administering to an individual in need thereof a drug-delivery composition of claim 1.
14:
- The method of claim 13, wherein said localized chronic inflammation disease is osteoarthritis.
15:
- The method of claim 13 wherein said composition is administered by intra-articular injection.
16:
- A pharmaceutical composition comprising:
- the drug delivery composition of claim 1, and (b) a pharmaceutically acceptable excipient and/or a carrier.
17:
- A drug-delivery composition comprising one or more microparticles, wherein each microparticle has non-spherical shape, and each microparticle is between about 1 and 100 μm in size, and said microparticle comprises at least one polymer and at least one inhibitor of C-C Chemokine Receptor-2 (CCR2).
18:
- The drug-delivery composition of claim 17, wherein each microparticle is in the shape of a prism.
19:
- The drug-delivery composition of claim 17, wherein the prism is a polyhedron comprising a first n-sided polygonal base, a second base which is a translated copy that is rigidly moved without rotation, and n other faces joining corresponding sides of the two bases, and the n other faces are parallelograms, wherein n is the number of sides of the polyhedron.
20:
- The drug-delivery composition of claim 19, wherein n is between about 3 and 8, or is 4.