Self-Nanoemulsifying Drug Delivery Systems Containing Plantago lanceolata-An Assessment of Their Antioxidant and Antiinflammatory Effects

• Published in: Molecules (Basel, Switzerland) Switzerland), 2017-10, Vol.22 (10), p.1773
• Main Authors: Kalantari, Azin, Kósa, Dóra, Nemes, Dániel, Ujhelyi, Zoltán, Fehér, Pálma, Vecsernyés, Miklós, Váradi, Judit, Fenyvesi, Ferenc, Kuki, Ákos, Gonda, Sándor, Vasas, Gábor, Gesztelyi, Rudolf, Salimi, Anayatollah, Bácskay, Ildikó
• Format: Article
• Language: English
• Subjects: Animals; Anti-Inflammatory Agents - administration & dosage; Anti-Inflammatory Agents - chemistry; Anti-Inflammatory Agents - pharmacology; antioxidant and anti-inflammatory effects; Antioxidants; Antioxidants - administration & dosage; Antioxidants - chemistry; Antioxidants - pharmacology; Bioactive compounds; Biocompatibility; Caco-2 Cells; Cell Survival - drug effects; Composition effects; Cytotoxicity; cytotoxicity investigation; Dilution; Dissolution; DPPH test; Drug delivery; Drug delivery systems; Ear Diseases - chemically induced; Ear Diseases - drug therapy; Edema; Edema - chemically induced; Edema - drug therapy; Emulsions; Humans; Hydrolysis; In vivo methods and tests; Inflammation; MTT-test; Nanoparticles - chemistry; Particle Size; Pharmacology; Physical properties; Plant Extracts - administration & dosage; Plant Extracts - chemistry; Plant Extracts - pharmacology; Plant Leaves - chemistry; Plant protection; Plantago - chemistry; Plantago lanceolata; SNEDDS; Statistical analysis; Statistical methods; Xylenes - adverse effects
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules22101773

The most important components of L. leaves are catalpol, aucubin, and acteoside (=verbascoside). These bioactive compounds possess different pharmacological effects: anti-inflammatory, antioxidant, antineoplastic, and hepatoprotective. The aim of this study was to protect extract from hydrolysis and to improve its antioxidant effect using self-nano-emulsifying drug delivery systems (SNEDDS). Eight SNEDDS compositions were prepared, and their physical properties, in vitro cytotoxicity, and in vivo AST/ALT values were investigated. MTT cell viability assay was performed on Caco-2 cells. The well-diluted samples (200 to 1000-fold dilutions) proved to be non-cytotoxic. The acute administration of PL-SNEDDS compositions resulted in minor changes in hepatic markers (AST, ALT), except for compositions and due to their high Transcutol contents (80%). The non-toxic compositions showed a significant increase in free radical scavenger activity measured by the DPPH test compared to the blank SNEDDS. An indirect dissolution test was performed, based on the result of the DPPH antioxidant assay; the dissolution profiles of extract were statistically different from each SNEDDS. The anti-inflammatory effect of PL-SNEDDS compositions was confirmed by the ear inflammation test. For the complete examination period, all compositions decreased ear edema as compared to the positive (untreated) control. It can be concluded that PL-SNEDDS compositions could be used to deliver active natural compounds in a stable, efficient, and safe manner.