Silymarin liposomes improves oral bioavailability of silybin besides targeting hepatocytes,and immune cells |
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| Institution: | 1. Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka, India;2. Manipal Acunova, Manipal, Karnataka, India;1. Department of Agricultural, Environmental and Food Sciences (DIAAA), University of Molise, via De Sanctis, Campobasso I-86100, Italy;2. Department of Life Sciences, University of Trieste, Trieste, TS I-34127, Italy;3. Department of Chemistry, University of Bari and CSGI, via Orabona 4, Bari 70126, Italy;4. Liver Unit, I.R.C.C.S. Casa Sollievo della Sofferenza Hospital, San Giovanni Rotondo, FG, Italy;5. Consorzio per lo sviluppo dei Sistemi a Grande Interfase (CSGI), Florence, Italy;1. Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, 31982 Al-Ahsa, Saudi Arabia;2. Department of Pharmacology, Faculty of Medicine, Minia University, 61511 El-Minia, Egypt;1. Dept. of Scienze della Vita e dell''Ambiente, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy;2. Institute of Science of Food Production UOS Sassari⿿CNR, Traversa la Crucca 3, Loc. Baldinca, 07040 Sassari, Italy;1. Institute of Food Science and Engineering, Hangzhou Medical College, Hangzhou 310007, Zhejiang, China;2. Reproductive Medicine Center, Jinhua People’s Hospital, Jinhua 321000, Zhejiang, China;3. Reproductive Medicine Center, Department of Reproductive Endocrinology, Zhejiang Provincial People’s Hospital, Affiliated People’s Hospital, Hangzhou Medical College, Hangzhou 310014, Zhejiang, China;1. Research Center for Biochemistry and Nutrition in Metabolic Diseases, Institute for Basic Sciences, Kashan University of Medical Sciences, Kashan, Iran;2. Student Research Committee, Kashan University of Medical Sciences, Kashan, Iran;3. Cancer Immunology Project (CIP), Universal Scientific Education and Research Network (USERN), Tehran, Iran;4. Department of Neurosurgery, School of Medicine, Baqiyatallah University of Medical Sciences, Tehran, Iran;5. Department of Gynecology and Obstetrics, School of Medicine, Shahid Beheshti University of Medical Sciences, Tehran, Iran;6. School of Medicine, Kashan University of Medical Sciences, Kashan, Iran;7. Department of Molecular Pharmacology, Albert Einstein College of Medicine, Bronx, NY 10463, USA;8. Department of Pharmacology, School of Medicine, Aja University of Medical Sciences, Tehran, Iran;9. Laser Research Centre, Faculty of Health Science, University of Johannesburg, Doornfontein 2028, South Africa;10. Toxicology Research Center, Aja University of Medical Sciences, Tehran, Iran;11. Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran |
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| Abstract: | BackgroundSilymarin, a hepatoprotective agent, has poor oral bioavailability. However, the current dosage form of the drug does not target the liver and inflammatory cells selectively. The aim of the present study was to develop lecithin-based carrier system of silymarin by incorporating phytosomal–liposomal approach to increase its oral bioavailability and to make it target-specific to the liver for enhanced hepatoprotection.MethodsThe formulation was prepared by film hydration method. Release of drug was assessed at pH 1.2 and 7.4. Formulation was assessed for in vitro hepatoprotection on Chang liver cells, lipopolysaccharide-induced reactive oxygen species (ROS) production by RAW 267.4 (murine macrophages), in vivo efficacy against paracetamol-induced hepatotoxicity and pharmacokinetic study by oral route in Wistar rat.ResultsThe formulation showed maximum entrapment (55%) for a lecithin–cholesterol ratio of 6:1. Comparative release profile of formulation was better than silymarin at pH 1.2 and pH 7.4. In vitro studies showed a better hepatoprotection efficacy for formulation (one and half times) and better prevention of ROS production (ten times) compared to silymarin. In in vivo model, paracetamol showed significant hepatotoxicity in Wistar rats assessed through LFT, antioxidant markers and inflammatory markers. The formulation was found more efficacious than silymarin suspension in protecting the liver against paracetamol toxicity and the associated inflammatory conditions. The liposomal formulation yielded a three and half fold higher bioavailability of silymarin as compared with silymarin suspension.ConclusionsIncorporating the phytosomal form of silymarin in liposomal carrier system increased the oral bioavailability and showed better hepatoprotection and better anti-inflammatory effects compared with silymarin suspension. |
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| Keywords: | Silymarin Liposome Phytosome Pharmacokinetic Paracetamol |
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