Telmisartan Self-Nanoemulsifying Drug Delivery System, Compared With Standard Telmisartan, More Effectively Improves Hepatic Fibrosis in Rats
| Autor: | Mamdooh Gari, Osama A. A. Ahmed, Tawfik M. Ghabrah, Hussam A. S. Murad |
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| Rok vydání: | 2020 |
| Předmět: |
Angiotensin receptor
Health Toxicology and Mutagenesis Liver fibrosis thioacetamide Pharmacology telmisartan Toxicology 030226 pharmacology & pharmacy Self nanoemulsifying 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine medicine liver fibrosis Chemical Health and Safety business.industry lcsh:RM1-950 Public Health Environmental and Occupational Health lcsh:Therapeutics. Pharmacology chemistry 030220 oncology & carcinogenesis Drug delivery Original Article Telmisartan Thioacetamide Hepatic fibrosis business medicine.drug |
| Zdroj: | Dose-Response Dose-Response, Vol 18 (2020) |
| ISSN: | 1559-3258 |
| DOI: | 10.1177/1559325820982190 |
| Popis: | Background:This study was designed to examine effects of telmisartan; an angiotensin receptor blocker; self-nanoemulsifying drug delivery system (SNEDDS) in reversing already-established hepatic fibrosis.Method:Forty rats were given thioacetamide (200 mg/kg, intraperitoneally) twice/week for 8 weeks then divided into 5 groups (n = 8), PC and 4 treated groups. Treatments were given orally for another 2 months as follows: telmisartan low and high doses (TL and TH: 1.8 and 3.6 mg/kg/day) and telmisartan SNEDDS at the same doses (TLS and THS). At end of treatment, blood was obtained and liver was isolated.Results:Rats showed significant elevations of plasma ALT and AST and hepatic IL-6, TNF-α, and MDA, significant reductions of plasma albumin, hepatic GSH, and body weight, and hepatic histopathological damage. All treatments except for TL significantly reversed these thioacetamide-induced changes. THS group showed significant differences from all groups. Regarding ratio of free telmisartan concentration in hepatic homogenate to that of plasma, TH and TLS groups showed non-significant variation between each other while THS group showed significant differences from them. No significant changes were detected in blood pressure, hemoglobin, white blood cells, and platelets.Conclusion:Telmisartan SNEDDS, compared with telmisartan, more effectively reversed chronic hepatic fibrosis with good safety profile. |
| Databáze: | OpenAIRE |
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