About this Research Topic
Resveratrol (3,5,4-trihydroxystilbene), a naturally occurring polyphenol, has been linked to many health promoting properties in Humans including anti-oxidant, anti-inflammatory, cardioprotective and antitumour activities. However, the development of therapeutic applications appears strongly limited by its low bioavailability in vivo. Indeed, in terms of physicochemical properties, trans-resveratrol is a fatsoluble compound, practically insoluble in water, and susceptible to UV-induced cis-isomerization with, loss of activity. Concerning its pharmacokinetics, resveratrol absorption rate is unusually high for a dietary polyphenol, but oral bioavailability of resveratrol is low because it is very rapidly metabolized in intestine and liver so that very low plasmatic levels of unchanged trans-resveratrol are observed. In this context, the increasing number of resveratrol formulation attempts reflects the major interest for developing pharmaceutical forms able to improve resveratrol bioavailability in the perspective of applying its therapeutic potentials in vivo.
Novel formulation approaches mainly based on multiparticulate forms and colloidal carriers were able to stabilize and protect resveratrol from degradation, to increase its solubility in water, in order to improve its bioavailability, and finally to achieve a sustained release and eventually to target resveratrol to specific locations. In addition, the research has also progressed regarding the control of resveratrol metabolism in order to improve its bioavailability. In addition, both increased intestinal permeation and modulation of presystemic metabolism of resveratrol could be achieved through self-emulsifying system formulation.
The present Research Topic proposes to make an overview of the recent innovations in terms of resveratrol formulation as well as metabolism modulation.
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