Effective Lipid Nanocarriers Based on Linseed Oil for Delivery of Natural Polyphenolic Active

Abstract

The main purpose of the present research was to test the ability of nanostructured lipid carriers (NLCs) to efficiently host a hydrophilic polyphenol active with health-promoting activities (caffeic acid (CA)). The caffeic acid-loaded lipid nanocarriers (CA-NLCs) were obtained by high-pressure homogenization technique using a surfactant mixture of Tween 20 and L-α-phosphatidylcholine in association with a lipid mixture of linseed oil, hexadecyl palmitate, and glycerol monostearate. In the first stage, the proportion between surfactant mixture and lipid phase has been varied to obtain appropriate stable nanocarriers. The optimized NLCs have been further loaded with different amounts of caffeic acid and were analyzed in terms of physical stability, size characteristics, and encapsulation efficiency. The antioxidant activity of CA-loaded NLCs and their release behavior have been tested by specific in vitro methods, e.g., ABTS (2,2-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid)) assay and release experiments, by Franz cell diffusion. The ABTS assay highlighted a high antioxidant potential of the caffeic acid in association with linseed oil. The capacity to capture ABTS cationic radicals was superior for the NLC entrapping an initial amount of 1.5% CA, the level of antioxidant capacity being 91.3%. The in vitro release experiments showed a different release behavior, depending on the initial amount of caffeic acid used. NLC loaded with a higher concentration of CA manifests a gradual slow release, e.g., 45% CA after 24 h of in vitro experiments, while the NLC loaded with smaller concentration of CA assured a higher release in time, around 65%.