Piperine: Old Spice and New Nutraceutical?

BACKGROUND: Many of the activities associated with pepper fruits have been attributed to piperine, the most active compound present in these spices. OBJECTIVE: This paper aims to provide an overview of the known properties of piperine, i.e. piperine's chemistry, its physiological activity, documented interactions as a bioenhancer and reported data concerning its toxicity, antioxidant properties and anticancer activity. DISCUSSION: It is known that piperine possesses several properties. In its interaction with other drugs, it can act as a bioavailability enhancer; this effect is also manifested in combination with other nutraceuticals, e.g. with curcumin, i.e. piperine can modify curcumin's antioxidant, anti-inflammatory, antimicrobial and anticancer effects. Piperine displays significant immunomodulating, antioxidant, chemopreventive and anticancer activity; these effects have been shown to be dose-dependent and tissue-specific. However, the main limitation associated with piperine seems to be its low bioavailability, a disadvantage that innovative formulations are overcoming. CONCLUSION: It is predicted that an increasing number of studies will focus on piperine, especially those directed towards unraveling its properties at molecular level. The current knowledge about the action of piperine will form a foundation for ways to improve piperine's bioavailability e.g. exploitation of different carrier systems. The therapeutical applications of this compound will be clarified, and piperine will be recognized as an important nutraceutical.

Contemporary Formulations for Drug Delivery of Anticancer Bioactive Compounds.

BACKGROUND: The immense development in the field of anticancer research has led to an increase in the research of bioactive compounds with anticancer potential. It has been known that many bioactive natural compounds have low solubility (and low bioavailability) as their main drawback when it comes to the formulation and drug delivery to specific sites. OBJECTIVE: As many attempts have been made to overcome this issue, this review gives a summary of the current accomplishments regarding the development of new Drug Delivery Systems (DDSs) represented by nanoparticles (NPs) and exosomes. METHODS: We analyzed the published data concerning selected compounds that present the most prominent plant secondary metabolites with anticancer potential, specifically flavone (quercetin), isoflavone (genistein and curcumin) and stilbene (resveratrol) groups that have been formulated as NPs and exosomes. In addition, we summarized the patent literature published from 2015-2018 that address these formulations. RESULTS: Although the exact mechanism of action for the selected natural compounds still remains unclear, the anticancer effect is evident and the main research efforts are directed to finding the most suitable delivery systems. Recent patents in this field serve as evidence that these newly designed natural compound delivery systems could be powerful new anticancer agents in the very near future if the noted difficulties are overcome. CONCLUSION: The focus of recent research is not only to clarify the exact mechanisms of action and therapeutic effects, but also to answer the issue of suitable delivery systems that can transport sufficient doses of bioactive compounds to the desired target.