Chapter 2 Herbal bioenhancers in microparticulate drug delivery

Review of microparticulate drug delivery unveils the boons that the system has to offer, yet only minimal knowledge of the role of herbal bioenhancers is available. Scientists focus intensely on ameliorating the bioavailability, while simultaneously downsizing adverse events to ensure safe drug delivery, directly drifting towards deploying plant-derived bioenhancers. Microparticulate drug delivery employs disintegrants and superdisintegrants for a sophisticated release, but dismally, hindrances such as the stagnant hydrophilic layer around a particle, the size of the drug particles released, and the P-glycoprotein efflux pumps pose complications to not only absorption but bioavailability as well. The bioenhancers that have been utilized in several novel drug deliveries have introduced serious compatibility and performance issues. Microparticulate drug delivery is best suited for use in plant bioenhancers such as quercetin, sinomenine, piperine, naringin, glycyrrhizin, genistein, and nitrile glycoside due to the simplified formulation and superlative stability. Modification of intestinal motility, stimulation of intestinal amino acid transporters, inhibition of cellular efflux pumps, inhibition of liver metabolism, and inhibition of intestinal enzymatic degradation are a handful of the proposed mechanisms. This chapter vividly puts forth the mechanisms and the studies on the use of plant bioenhancers for microparticulate drug delivery, the regulatory concerns, and the prospects in this discipline.