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

Dina Guzmán-Oyarzo,Dulcineia S P Abdalla,Jacobo Hernández-Montelongo,Luis A Salazar,Gonzalo Recio-Sánchez,Tanya Plaza

doi:10.3390/pharmaceutics11060289

Dina Guzmán-Oyarzo, Dulcineia S P Abdalla + Show 4 more

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https://doi.org/10.3390/pharmaceutics11060289

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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.

Highlights

Since ancient times, the use of natural compounds has been of great importance for medicine mainly in the prevention and treatment of different pathologies [1,2]
For the Brazilians propolis, Daleprane et al [9] reported that artepellin C, pinocembrin and kampferol were the main components of green propolis; 3-hydroxy-8,9-dimethoxypterocarpane, medicarpine and daidezein were the main components of red propolis; and pinocembrin, phenyl ester of caffeic acid, quercetin and galangin were the main components of brown propolis
The aim of this work is to determine if nanoporous silicon (nPSi)-βCD microparticles are a suitable and safe 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

Summary

Introduction

The use of natural compounds has been of great importance for medicine mainly in the prevention and treatment of different pathologies [1,2]. An example of natural compounds with bioactive potential is propolis, which is a resinous compound produced by bees from plants exudates Studies both in vitro and in vivo have identified a wide variety of biological activities for propolis: antibacterial [4], antifungal [5], antioxidant [6], anti-inflammatory [7], anti-carcinogenic [8] and anti-angiogenic [9]. Concerning to the presence and abundance of polyphenols in propolis, they are very variable due to their close dependence with the botanical origin of plants, climate, geographical location, year and time of collection [3,18,19] Examples of this important dependence are the studies of three Brazilians, one Polish and one Chilean propolis. For the Chilean propolis with anti-atherogenic and anti-angiogenic activity [21], the main polyphenols detected in the ethanolic extract were caffeic acid (a phenolic acid) and pinocembrin (a flavonone) [22]

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