Extended osteoarthritis pain relief with neosaxitoxin using alginate-core polymeric microparticles
Abstract
-glycolic acid) microparticles (AlgPLGA-MPs). Incorporation of a negatively charged alginate core in the inner aqueous phase enhanced NSTX encapsulation through electrostatic interactions and minimized burst release. IA injection of NSTX encapsulated AlgPLGA-MP in a murine OA model produced significant pain relief for up to one week. To further prolong joint residence time, the microparticle surface was functionalized with cationic avidin (AvAlgPLGA-MP) that reversed the net surface charge from anionic to cationic. This modification promoted electrostatic binding to negatively charged synovial matrix components and prolonged intra-joint retention time, while maintaining biocompatibility. Together, these results establish NSTX as a highly potent analgesic for chronic OA pain and present alginate-core PLGA microparticles as a safe and effective sustained-release platform. This delivery system holds broad translational potential for other small, hydrophilic analgesics and therapeutic agents.
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