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- Title
Nanostructured Lipid Carriers as Promising Delivery Systems for Plant Extracts: The Case of Silymarin.
- Authors
Piazzini, Vieri; Lemmi, Beatrice; D’Ambrosio, Mario; Cinci, Lorenzo; Luceri, Cristina; Bilia, Anna Rita; Bergonzi, Maria Camilla
- Abstract
Featured Application: <bold>Silymarin, a standardized extract derived from seeds and fruits of <italic>Silybum marianum</italic> L. Gaertn., is widely used for treatment of various acute and chronic liver toxicities, inflammation, fibrosis and oxidative stress. The extract has low toxicity and exerts significant anti-carcinogenic and anti-inflammatory effects. Recently, it has been reported that the extract is beneficial in type 2 diabetes patients. However, Silymarin is a low water soluble and low permeable compound, belonging to biopharmaceutical class IV type that faces stipulated requirements in delivery design. Thus, to overcome these limitations, the extract was encapsulated into nanostructured lipid carriers. The lipid nanocarriers offer potential applications as natural, low cost and innovative delivery systems to improve solubility, permeability and stability of extract. Other advantages are: possibility of controlled drug release and drug targeting, no biotoxicity of the carrier, biodegradation and no problems with respect to scale-up production in the food and pharmaceutical fields.</bold> Background: Silymarin is the extract from seeds of <italic>Silybum marianum</italic> L. Gaertn. and it has been used for decades as hepatoprotectant. Recently, it has been proposed to be beneficial in type 2 diabetes patients. However, silymarin is a poorly water soluble drug with limited oral bioavailability. In this study, nanostructured lipid carriers were proposed to enhance its solubility and intestinal absorption. Methods: Nanostructured lipid carriers were made of Stearic acid:Capryol 90 as lipid mixtures and Brij S20 as surfactant. Formulations were physically and chemically characterized. Stability and in vitro release studies were also assessed. In vitro permeability and Caco-2 cellular uptake mechanism were investigated. Results: Obtained results were based on size, homogeneity, ζ-potential and EE%. Nanostructured lipid carriers could be orally administered. No degradation phenomena were observed in simulated gastrointestinal fluids. Storage stability of suspensions and lyophilized products was also tested. Glucose was selected as best cryoprotectant agent. About 60% of silymarin was released in 24 h in phosphate buffered saline. In vitro parallel artificial membrane permeability assay experiments revealed that the nanocarrier enhanced the permeation of Silymarin. Caco-2 study performed with fluorescent nanoparticles revealed the ability of carrier to enhance the permeation of a lipophilic probe. Cellular uptake studies indicated that active process is involved in the internalization of the formulation. Conclusions: The optimized nanostructured lipid carriers showed excellent chemical and physical stability and enhanced the absorption of silymarin.
- Subjects
NANOSTRUCTURED materials; LIPIDS
- Publication
Applied Sciences (2076-3417), 2018, Vol 8, Issue 7, p1163
- ISSN
2076-3417
- Publication type
Article
- DOI
10.3390/app8071163