Improved in vitro and in vivo hepatoprotective effects of liposomal silymarin in alcohol-induced hepatotoxicity in Wistar rats |
| |
| Affiliation: | 1. Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India;2. Ecron Acunova Limited, Manipal, Karnataka, India;3. Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India;4. Ranbaxy Laboratories Limited, Gurgaon, India;1. Department of Internal Medicine and Clinical Pharmacology, Medical University of Silesia, Katowice, Poland;2. Department of Paediatrics in Bytom, School of Health Sciences in Katowice, Medical University of Silesia, Katowice, Poland;3. Gyncentrum Fertility Clinic, Katowice, Poland;1. Department of Clinical and Experimental Medicine, University of Pisa, Pisa, Italy;2. Department of Surgical, Medical and Molecular Pathology and Critical Care Medicine, University of Pisa, Pisa, Italy;3. Department of Pharmacy, University of Pisa, Pisa, Italy;1. Department of Experimental and Clinical Pharmacology, Medical University of Warsaw, Centre for Preclinical Research and Technology CePT, Warszawa, Poland;2. Department of Neurology of the Second Faculty of Medicine, Medical University of Warsaw, Warszawa, Poland;3. 2nd Department of Neurology, Institute of Psychiatry and Neurology, Warszawa, Poland;1. Research Center of Natural Resources of Chinese Medicinal Materials and Ethnic Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang, PR China;2. Department of Chemical and Pharmaceutical Engineering, College of Chemical Engineering, Huaqiao University, Xiamen, 361021, Fujian Province, PR China;1. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA), CONICET - Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Córdoba, Argentina;2. Facultad de Ciencias Médicas, Universidad Nacional de Córdoba. Ciudad Universitaria, Córdoba, Argentina;1. Department of Pharmacology and Toxicology, Faculty of Medicine, University of Warmia and Mazury, Olsztyn, Poland;2. Department of Biochemistry and Toxicology, Faculty of Biology, Animal Sciences and Bioeconomy, University of Life Sciences in Lublin, Lublin, Poland;3. Division of Food Science, Institute of Animal Reproduction and Food Research, Polish Academy of Sciences, Olsztyn, Poland |
| |
| Abstract: | BackgroundSilymarin, a known hepatoprotectant, owing to its poor oral bioavailability, has limited pharmacological effects. The present study was designed to improve its in vitro and in vivo hepatoprotection and increase its oral bioavailability against alcohol intoxication by formulating it in four different liposomal formulations namely conventional, dicetyl phosphate, stearyl amine and PEGylated liposomes.MethodThe liposomes were prepared using phosphatidylcholine, cholesterol, and silymarin in addition to dicetyl phosphate, stearyl amine and DSPE mPEG 2000 by film hydration method with 5% sucrose as a cryo-protectant. The optimized formulations were studied for their release profile at pH 1.2 and 6.8. Liposomes were studied for in vitro protection on Chang liver cells and efficacious liposomes were selected for in vivo hepatoprotection study. Further, conventional liposomes were studied for bioavailability in alcohol intoxicated Wistar rats.ResultsThe conventional liposomes increased in vitro release profile at pH 1.2 and 6.8 and also showed better in vitro protection compared to silymarin alone. Conventional and PEGylated liposomes showed better improvement in liver function, better efficacy in combating inflammatory conditions, better improvement in antioxidant levels and reversal of histological changes compared to silymarin alone. Conventional also showed an almost fourfold increase in area under the curve compared to silymarin suspension.ConclusionConventional and PEGylated liposomes of silymarin were found to be more efficacious as hepatoprotective against alcohol-induced hepatotoxicity by its free radical scavenging and anti-inflammatory effects. Conventional liposomes showed enhanced bioavailability compared to silymarin alone. |
| |
| Keywords: | Silymarin Alcohol Liposomes Hepatoprotection PEGylated liposomes |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
