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.

Geographic Area of Collection Determines the Chemical Composition and Antimicrobial Potential of Three Extracts of Chilean Propolis

“…Quercetin-3-glucuronide, a derivative of quercetin, and quercetin and isorhamnetin, can affect the transduction process of nuclear factor NF-kB, and consequently can decrease Nrf2 gene expression and allow the inactivation of miR-155 with pro-inflammatory activity [ 34 ]. Individual polyphenols such as CAPE, pinocembrin and apigenin can act on breast cancer cells, with antioxidant and anti-angiogenic properties [ 35 , 36 , 37 ].…”

Controlled Release of Caffeic Acid and Pinocembrin by Use of nPSi-βCD Composites Improves Their Antiangiogenic Activity

“…nPSi-βCD composite microparticles were synthesized following a method previously reported [ 38 ]. Si wafers were cleaned by ultrasonication in acetone, isopropanol, and distilled water.…”

“…The loading and release of polyphenols using nPSi-βCD composites microparticles were obtained following a method previously reported [ 38 ]. Polyphenols CA and Pin were reconstituted with 100% DMSO and stored at −20 °C until required.…”

“…Thus, from the available evidence, the general aim of this study is to evaluate, in vitro, the antiangiogenic and antioxidant effects of the polyphenols caffeic acid and pinocembrin in solution and microencapsulated using nPSi-βCD composites. These composite microparticles were recently developed by our group using nanoporous silicon (nPSi), chitosan, and a β-cyclodextrin polymer (βCD polymer) [ 38 ]. We studied their use for the controlled release of both caffeic acid and pinocembrin, two main polyphenolic compounds found in Chilean propolis.…”

Functional Polymers for Controlled Drug Release

“…The transport and sustained release of bioactive polyphenols, usually extracted from plants or food, was also dealt with by Guzman-Oyarzo et al [5]. In order to avoid degradation reactions of these bioactive molecules, the authors proposed a synthetic strategy involving a flexible and soft β-ciclodextrin polymer within the highly porous inorganic matrix of nanoporous silicon [6] as a substrate.…”