Nanoformulations of pazopanib, compositions comprising the same and methods of treating osteoarthritis
Inventors
Sampen, Hee-Jeong Im • Liu, Ying
Assignees
United States Department of Veterans Affairs • University of Illinois System
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Publication Number
US-12678411-B2
Publication Date
2026-07-14
Expiration Date
Abstract
Disclosed herein are nanoparticles comprising Pazopanib or a derivative thereof encapsulated by the copolymer poly (lactic-co-glycolic acid) (PLGA). Also disclosed herein are methods for treating osteoarthritis, inhibiting or preventing cartilage degeneration, and reducing or inhibiting pain-associated depression in subjects with joint pain with nanoparticles comprising Pazopanib or a derivative thereof.
Core Innovation
The invention relates to nanoparticle nanoformulations of the VEGFR1/VEGFR2 inhibitor pazopanib and pazopanib derivatives encapsulated by poly (lactic-co-glycolic acid) (PLGA) and/or poly (ethylene glycol)-b-polycaprolactone (PEG-b-PCL). The nanoparticle is further provided in a pegylated liposome form, combining polymer encapsulation with a pegylated liposome presentation.
The invention addresses osteoarthritis (OA), in which Flt1 is implicated in pain transmission and Flk1 contributes to cartilage degeneration. The pazopanib-containing nanoparticle formulations are described for inhibiting cartilage degeneration and reducing joint pain, including effects connected to pain-associated depression and modulation of the spinal NF-κB/glial activation axis.
The described nano-PAZ formulations, including nano-PAZ I, nano-PAZ II, and nano-PAZ III, support prolonged pain relief and cartilage protection after single-dose intraarticular administration. The disclosure includes combination with mesenchymal stem cells and optional formulation variants such as pegylation, pegylated liposome coatings, cryoprotective agents, and positively charged components.
Claims Coverage
The partial content provides one independent claim. The independent claim covers one core inventive composition feature and one presentation feature.
Pazopanib encapsulated nanoparticle in a pegylated liposome form
A nanoparticle comprising or consisting of Pazopanib encapsulated by poly (lactic-co-glycolic acid) (PLGA), poly (ethylene glycol)-b-poly (e-caprolactone) (PEG-b-PCL), or a combination thereof, wherein the nanoparticle is in a pegylated liposome.
The disclosed refinements add composition and formulation limitations, including nanoparticle size and Pazopanib amount/PLGA-to-pazopanib ratio, and optional components such as cryoprotective agent and positively charged components, together with therapeutic use and intraarticular administration details and optional co-administration with mesenchymal stem cells.
Stated Advantages
Prolonged pain relief after single-dose intraarticular administration.
Cartilage protection after single-dose intraarticular administration.
Inhibition of cartilage degeneration.
Reduction of joint pain.
Addressing OA-associated pain, including pain-associated depression.
Modulation of the spinal NF-κB/glial activation axis.
Documented Applications
Intraarticular treatment of osteoarthritis (OA), including inhibition of cartilage degeneration and reduction of joint pain after single-dose IA administration.
Use in addressing OA-associated pain-associated depression and modulation of the spinal NF-κB/glial axis.
Combination with mesenchymal stem cells in osteoarthritis-related therapeutic use.
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