Use of nPSi-βCD Composite Microparticles for the Controlled Release of Caffeic Acid and Pinocembrin, Two Main Polyphenolic Compounds Found in a Chilean Propolis

Abstract

Propolis is widely recognized for its various therapeutic properties. These are attributed to its rich composition in polyphenols, which exhibit multiple biological properties (e.g., antioxidant, anti-inflammatory, anti-angiogenic). Despite its multiple benefits, oral administration of polyphenols results in low bioavailability at the action site. An alternative to face this problem is the use of biomaterials at nano-micro scale due to its high versatility as carriers and delivery systems of various drugs and biomolecules. The aim of this work is to determine if nPSi-βCD microparticles are a suitable material for the load and controlled release of caffeic acid (CA) and pinocembrin (Pin), two of the main components of a Chilean propolis with anti-atherogenic and anti-angiogenic activity. Polyphenols and nPSi-βCD microparticles cytocompatibility studies were carried out with human umbilical vein endothelial cells (HUVECs). Results from physicochemical characterization demonstrated nPSi-βCD microparticles successfully retained and controlled release CA and Pin. Furthermore, nPSi-βCD microparticles presented cytocompatibility with HUVECs culture at concentrations of 0.25 mg/mL. These results suggest that nPSi-βCD microparticles could safely be used as an alternate oral delivery system to improve controlled release and bioavailability of CA or Pin—and eventually other polyphenols—thus enhancing its therapeutic effect for the treatment of different diseases.

Keywords

• controlled release
• nanoporous silicon
• βCD polymer
• caffeic acid
• pinocembrin
• polyphenols
• HUVECs