PPF microsphere depot sustains NSAID blood levels with infusion‐like kinetics without ‘burst’

Abstract

Management of pain is of paramount importance for a myriad of indications in human and animal health. Unfortunately, the administration of pain therapeutics is often complicated by insufficient control over pharmacokinetic profiles as a result of frequent oral dosing. Attempts to sustain and tightly control the concentration of these drugs in the blood via controlled release injectable formulations have typically resulted in drug 'burst', followed by marginal control over the ensuing pharmacokinetics. Here, precision particle fabrication (PPF) technology was used to produce uniform microspheres encapsulating the nonsteroidal anti-inflammatory drug meloxicam. After subcutaneous injection, plasma concentrations of meloxicam were held constant in canines for more than 2 weeks without initial drug burst. Pharmacokinetic profiles were accurately modeled using equations typically applied to steady-state infusion. PPF microsphere depots of pain therapeutics or other compounds may ultimately improve safety and sustain the efficacy of medications where such controlled uniform exposure would be therapeutically beneficial.