Application of Spray Drying Particle Engineering to a High-Functionality/Low-Solubility Milk Thistle Extract: Powders Production and Characterization

• Published in: Molecules (Basel, Switzerland) Vol. 23; no. 7; p. 1716
• Main Authors: Sansone, Francesca, Esposito, Tiziana, Lauro, Maria Rosaria, Picerno, Patrizia, Mencherini, Teresa, Gasparri, Franco, De Santis, Stefania, Chieppa, Marcello, Cirillo, Claudia, Aquino, Rita Patrizia
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 14.07.2018; MDPI
• Subjects: Animals; anti-inflammatory activity; Biological activity; Carboxymethylcellulose Sodium - chemistry; Carboxymethylcellulose Sodium - pharmacology; Dendritic Cells - cytology; Dendritic Cells - metabolism; functional stability; in vitro dissolution and permeation tests; Mice; Plant Extracts - chemistry; Plant Extracts - pharmacology; Powders; Silybum marianum - chemistry; Silymarin - chemistry; Silymarin - pharmacology; silymarin complex; water solubility; in vitro dissolution and permeation tests; silymarin complex; water solubility; functional stability; anti-inflammatory activity
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules23071716

Many natural compounds having antioxidant and anti-inflammatory activity are a potential target for new therapies against chronic inflammatory syndromes. The oral administration of functional herbal supplements may become a prevention strategy or therapy adjuvant for susceptible patients. A case study is our milk thistle (Silybum marianum) extract rich in silymarin complex. A water-soluble microencapsulated powder system was developed by a spray drying technique to improve the poor silymarin bioactivity after oral administration. Sodium carboxymethylcellulose (NaCMC) was employed as coating/swelling polymer matrix and sodium lauryl sulfate (SLS) as the surfactant (1:1:0.05 w/w/w). A H2O/EtOH/acetone (50/15/35 v/v/v) solvent system was used as liquid feed. The microsystems were capable of improving the in vitro dissolution and permeation rates, suggesting an enhancement of bioactivity after oral administration. The microsystems protect the antioxidant activity of silymarin after harsh storage conditions period and do not affect the anti-inflammatory properties of the raw extract (efficient already at lower concentrations of 0.312 mg/mL) to reduce dendritic cells (DCs) inflammatory cytokine secretion after lipopolysaccharide administration. This approach allows managing particle size, surface properties and release of bioactive agents improving the bioactivity of a herbal supplement and is also possibly applicable to many other similar natural products.