POLYSULFONE BASED CORE:SHELL MICOSPHERES FOR INTRASPINAL DELIVERY OF GABAPENTIN
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Date
2023-05
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The Ohio State University
Abstract
Spinal cord injury is a devastating injury that often results in chronic neuropathic pain, from
overactive nociceptors, and some degree of paralysis below the injury site. With almost 70% of spinal
cord injuries resulting from motor-vehicle accidents or falls, it is pertinent that a novel medical
intervention is developed to restore quality of life. Voltage gated calcium channels have been found to
mediate nociceptors and specifically, expression α2δ1/2 subunits of voltage gated calcium channels have
been found to downregulate axon regeneration and growth. Gabapentin has been targeted as a possible
treatment because it reduces the excitability of neurons but large oral doses are required to prove
effective, resulting in unwanted side effects such as nausea and swelling of extremities. Prior research
done by our group has proved that localized injections of gabapentin forms a pharmacological blockade
at voltage gated calcium channels, particularly α2δ1/2 subunits, promoting axon regrowth and
regeneration; thus, improving functional recovery in patients suffering from spinal cord injury. Novel
polysulfone based electrosprayed core:shell microparticles with diameters of ~1um were used to
encapsulate gabapentin, allowing localized administration of gabapentin without the need for systemic
injections. Microparticles with Pluronic F-127 in the 'shell' exhibited a porous or dimpled surface
morphology with small fibrils while microparticles without F-127 in the 'shell' exhibited a smooth
surface morphology with some globular formations. In vitro pharmaceutical release assays showed that
particles with F-127 in the shell would release gabapentin for nearly 10-14 days at ~0.3wt%/hr
following an initial burst release. Further characterization and optimization of the polysulfone core:shell
particles should be pursued to improve release kinetics of particle to better benefit patients suffering
from spinal cord injuries.
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Keywords
Polymers, Spinal cord Injury, Drug delivery, Micro-particles