Abstract
This study offers a novel oral pregabalin (PG)-loaded drug delivery system based on chitosan and hypromellose phthalate-based polymeric nanocomposite in order to treat neuropathic pain (PG-PN). PG-PN has a particle size of 432 ± 20 nm, a polydispersity index of 0.238 ± 0.001, a zeta potential of +19.0 ± 0.9 mV, a pH of 5.7 ± 0.06, and a spherical shape. Thermal and infrared spectroscopy confirmed nanocomposite generation. PG-PN pharmacokinetics was studied after a single oral dose in male Wistar rats. PG-PN showed greater distribution and clearance than free PG. The antinociceptive effect of PG-PN in neuropathic pain rats was tested by using the chronic constriction injury model. The parameter investigated was the mechanical nociceptive threshold measured by the von Frey filaments test; PG-PN showed a longer antinociceptive effect than free PG. The rota-rod and barbiturate sleep induction procedures were used to determine adverse effects; the criteria included motor deficit and sedative effects. PG-PN and free PG had plenty of motors. PG-PN exhibited a less sedative effect than free PG. By prolonging the antinociceptive effect and decreasing the unfavorable effects, polymeric nanocomposites with pregabalin have shown promise in treating neuropathic pain.
Highlights
Pregabalin (PG) (S-[+]-3-isobutyl GABA or (S)-3-aminomethyl-5-methylhexanoic acid) is an anticonvulsant, antihyperalgesic, and anxiolytic drug that acts by binding to the alpha-2-delta-1 proteins of voltage-dependent calcium channels in the Central Nervous System (CNS), reducing the release of excitatory neurotransmitters [1]
PG is a class I molecule with good solubility and permeability, according to the Biopharmaceutical Classification System (BSC) [6], indicating that it has no physicochemical issues that would require a change in pharmaceutical form
The average particle size of Pregabalin-Loaded Polymeric Nanocomposite (PG-polymeric nanocomposites (PN)) was determined using the Dynamic light scattering (DLS) method, PdI, and the zeta potential of tests were performed with Statistica 7.0 (StatSoft Power Solutions, Inc., Hamburg, Germany); the threshold of significance for all statistical tests was set at 5%
Summary
Pregabalin (PG) (S-[+]-3-isobutyl GABA or (S)-3-aminomethyl-5-methylhexanoic acid) is an anticonvulsant, antihyperalgesic, and anxiolytic drug that acts by binding to the alpha-2-delta-1 proteins of voltage-dependent calcium channels in the Central Nervous System (CNS), reducing the release of excitatory neurotransmitters [1]. PG is one of the first-choice medicines for the treatment of neuropathic pain that has been authorized by the FDA [2]. Due to its short half-life, PG is sold as an instant release (IR) tablet, with a daily dosage of 150 to 600 mg split into two or three administrations [1,3]. Sleepiness, dizziness, and loss of consciousness are common adverse effects of PG [1]. Around 15% of patients using pregabalin for neuropathic pain discontinue their therapy due to adverse effects, even when the dosages are tolerable [4,5]. As neuropathic pain is persistent and needs lengthy therapy, these two variables (short half-life and adverse effects) might be a barrier for appropriate treatment compliance [3]
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