Abstract
BackgroundThe fatty acid amide palmitoylethanolamide (PEA) has been studied extensively for its anti-inflammatory and neuroprotective actions. The lipidic nature and large particle size of PEA in the native state may limit its solubility and bioavailability when given orally, however. Micronized formulations of a drug enhance its rate of dissolution and reduce variability of absorption when orally administered. The present study was thus designed to evaluate the oral anti-inflammatory efficacy of micronized/ultramicronized versus nonmicronized PEA formulations.MethodsMicronized/ultramicronized PEA was produced by the air-jet milling technique, and the various PEA preparations were subjected to physicochemical characterization to determine particle size distribution and purity. Each PEA formulation was then assessed for its anti-inflammatory effects when given orally in the carrageenan-induced rat paw model of inflammation, a well-established paradigm of edema formation and thermal hyperalgesia.ResultsIntraplantar injection of carrageenan into the right hind paw led to a marked accumulation of infiltrating inflammatory cells and increased myeloperoxidase activity. Both parameters were significantly decreased by orally given micronized PEA (PEA-m; 10 mg/kg) or ultramicronized PEA (PEA-um; 10 mg/kg), but not nonmicronized PeaPure (10 mg/kg). Further, carrageenan-induced paw edema and thermal hyperalgesia were markedly and significantly reduced by oral treatment with micronized PEA-m and ultramicronized PEA-um at each time point compared to nonmicronized PeaPure. However, when given by the intraperitoneal route, all PEA formulations proved effective.ConclusionsThese findings illustrate the superior anti-inflammatory action exerted by orally administered, micronized PEA-m and ultramicronized PEA-um, versus that of nonmicronized PeaPure, in the rat paw carrageenan model of inflammatory pain.
Highlights
The fatty acid amide palmitoylethanolamide (PEA) has been studied extensively for its antiinflammatory and neuroprotective actions
The results demonstrate that micronized/ultramicronized PEA has a significantly improved anti-inflammatory and antihyperalgesic profile compared to nonmicronized PEA when given by the oral route
Because increasing a drug’s surface area enhances its rate of dissolution [14] while reducing variability of absorption [15], we investigated the influence of micronization/ ultramicronization on PEA action in carrageenan-induced inflammation in the rat paw
Summary
The fatty acid amide palmitoylethanolamide (PEA) has been studied extensively for its antiinflammatory and neuroprotective actions. The lipidic nature and large particle size of PEA in the native state may limit its solubility and bioavailability when given orally, . Micronized formulations of a drug enhance its rate of dissolution and reduce variability of absorption when orally administered. The present study was designed to evaluate the oral anti-inflammatory efficacy of micronized/ultramicronized versus nonmicronized PEA formulations. Nonresolving inflammation is one of the principal contributors to the medical burden in industrialized societies. Neuroinflammation in both the peripheral and central nervous systems plays an important role in the pathogenesis of chronic pain [3,4]. Therapeutic targeting of the inflammatory response continues to be an area of intense research activity
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