Estudo do encapsulamento e da liberação de quercetina em sistemas lipídicos: efeitos de carga e rigidez

Abstract

Quercetin is a bioactive that has a wide range of applications, but its use for pharmacological purposes presents difficulties related to its low bioavailability and solubility in aqueous media, high propensity to degradation by light, heat and oxygen, as well as its reduced biological activity. in the gastrointestinal tract. A powerful strategy to enhance its biological activity is to encapsulate it in nanoparticulate and microparticulate systems. MLVs (multilamellar vesicles) represent a suitable low cost alternative to encapsulate hydrophobic bioactive molecules being successfully used in several areas. Due to the versatility in the preparation of MLVs and considering the variety of lipids and sterols found in nature, we investigated the effect of different lipid compositions in the manufacture of MLVs for encapsulation and controlled release of quercetin. In order to do so, the effects of load and stiffness on the average size of the formulation, size distribution, load properties and the encapsulation efficiency and release of this polyphenol were considered. Our results demonstrated that the rigidity imposed by Colesterol increased both the homogeneity of the size distribution and the encapsulation efficiency enabling a significant rate of quercetin release at the system with 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoColine/Colesterol (80:20). The charge modulated both the average size and size distribution as well as resulted in high encapsulation and release efficiencies in the formulation composed of (1-palmitoyl-2-oleoyl-sn-glycero-3-phosphoColine/1-palmitoyl-2-oleoyl-sn-glycero-3-phosphatidylglycerol (80:20). To the best of our knowledge, this is the first study concerning charge and rigidity effects on the encapsulation of quercetin in multilamellar vesicles, with great potential for technological application. Furthermore, the news presented in this work is a starting point on the use of lipid composition as a modulating agent of important parameters in the development of nano and micro systems.