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Preparation and in vitro–in vivo evaluation of sustained-release matrix pellets of capsaicin to enhance the oral bioavailability

Capsaicin has multiple pharmacological activities including antioxidant, anticancer, and antiinflammatory activities. However, its clinical application is limited due to its poor aqueous solubility, gastric irritation, and low oral bioavailability. This research was aimed at preparing sustained-release matrix pellets of capsaicin to enhance its oral bioavailability. The pellets comprised of a core of soliddispersed capsaicin mixed with microcrystalline cellulose (MCC) and hydroxypropyl cellulose (HPMC) and subsequently coating with ethyl cellulose (EC) were obtained by using the technology of extrusion/ spheronization. The physicochemical properties of the pellets were evaluated through scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD). | Preparation and in vitro in vivo evaluation of sustained-release matrix pellets of capsaicin to enhance the oral bioavailability