Marwa Khaled Mohsen, Soheir Abo El azm Diab, Amani N. Shafik, Ahmed H. Osman, Marianne J. Naguib, Amira M. Kamel, Marwa Nagi Mehesen
{"title":"索非布韦在大鼠中的肝保护作用通过包封在牛磺酸胆酸稳定的半乳糖锚定的胆小体中而增强","authors":"Marwa Khaled Mohsen, Soheir Abo El azm Diab, Amani N. Shafik, Ahmed H. Osman, Marianne J. Naguib, Amira M. Kamel, Marwa Nagi Mehesen","doi":"10.1186/s43094-025-00775-w","DOIUrl":null,"url":null,"abstract":"<div><h3>Background</h3><p>In conjunction with other antiviral medicines, sofosbuvir (SOF) is an essential therapy for chronic hepatitis C. There is some debate over its influence on hepatic fibrosis. The use of nanotechnology in treatment has gained popularity, with the goal of delivering therapeutic substances to the liver to increase efficacy and decrease adverse effects. The aim of this study was to demonstrate the protective effect of sofosbuvir and the efficacy of incorporating nanoparticle galactosylated taurocholate bilosomal formula to SOF on thioacetamide-induced liver fibrosis.</p><h3>Methods</h3><p>Rats were divided into 7 groups: normal control, SOF, SOF encapsulated in galactosylated taurocholate bilosomal formula (nano-SOF), galactosylated taurocholate bilosomal formula (nanoparticle), thioacetamide (TAA), TAA-SOF and TAA-nano-SOF. Liver fibrosis was induced by TAA (200 mg/kg) intraperitoneal injection twice per week for 8 weeks. SOF, nanoparticle and nano-SOF were given (40 mg/Kg/day) orally from day one of the study. Serum activities of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP) and tissue transforming growth factor beta (TGF-<i>β</i>) were assessed. Also, histopathological assessment of hepatic tissue was done.</p><h3>Results</h3><p>Administration of SOF and TAA to normal rats resulted in significant increase in serum AST, ALT, ALP and tissue TGF-β<sub>1</sub> levels with variable degree of liver fibrosis. Additionally, rats in TAA group that received SOF therapy did not exhibit improved liver functions, TGF-β<sub>1</sub> level and liver fibrosis score. However, administering nano-sofosbuvir prophylactically to TAA-treated rats resulted in a considerable improvement in liver function tests, TGF-1 levels, with liver fibrosis score regression.</p><h3>Conclusion</h3><p>In contrast to free sofosbuvir, SOF encapsulated in galactosylated taurocholate bilosomal formula (nano-SOF) displayed hepatoprotective effects in rat with thioacetamide-induced hepatic fibrosis. These findings strongly support the concept that galactoylatedbilosomes are promising nanocarrier for the targeted delivery of sofosbuvir to the liver.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":3.4000,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-025-00775-w","citationCount":"0","resultStr":"{\"title\":\"Sofosbuvir’s hepatoprotective efficacy in rats is enhanced by encapsulating in taurocholate-stabilized galactose-anchored bilosomes\",\"authors\":\"Marwa Khaled Mohsen, Soheir Abo El azm Diab, Amani N. Shafik, Ahmed H. Osman, Marianne J. Naguib, Amira M. Kamel, Marwa Nagi Mehesen\",\"doi\":\"10.1186/s43094-025-00775-w\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Background</h3><p>In conjunction with other antiviral medicines, sofosbuvir (SOF) is an essential therapy for chronic hepatitis C. There is some debate over its influence on hepatic fibrosis. The use of nanotechnology in treatment has gained popularity, with the goal of delivering therapeutic substances to the liver to increase efficacy and decrease adverse effects. The aim of this study was to demonstrate the protective effect of sofosbuvir and the efficacy of incorporating nanoparticle galactosylated taurocholate bilosomal formula to SOF on thioacetamide-induced liver fibrosis.</p><h3>Methods</h3><p>Rats were divided into 7 groups: normal control, SOF, SOF encapsulated in galactosylated taurocholate bilosomal formula (nano-SOF), galactosylated taurocholate bilosomal formula (nanoparticle), thioacetamide (TAA), TAA-SOF and TAA-nano-SOF. Liver fibrosis was induced by TAA (200 mg/kg) intraperitoneal injection twice per week for 8 weeks. SOF, nanoparticle and nano-SOF were given (40 mg/Kg/day) orally from day one of the study. Serum activities of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP) and tissue transforming growth factor beta (TGF-<i>β</i>) were assessed. Also, histopathological assessment of hepatic tissue was done.</p><h3>Results</h3><p>Administration of SOF and TAA to normal rats resulted in significant increase in serum AST, ALT, ALP and tissue TGF-β<sub>1</sub> levels with variable degree of liver fibrosis. Additionally, rats in TAA group that received SOF therapy did not exhibit improved liver functions, TGF-β<sub>1</sub> level and liver fibrosis score. 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Sofosbuvir’s hepatoprotective efficacy in rats is enhanced by encapsulating in taurocholate-stabilized galactose-anchored bilosomes
Background
In conjunction with other antiviral medicines, sofosbuvir (SOF) is an essential therapy for chronic hepatitis C. There is some debate over its influence on hepatic fibrosis. The use of nanotechnology in treatment has gained popularity, with the goal of delivering therapeutic substances to the liver to increase efficacy and decrease adverse effects. The aim of this study was to demonstrate the protective effect of sofosbuvir and the efficacy of incorporating nanoparticle galactosylated taurocholate bilosomal formula to SOF on thioacetamide-induced liver fibrosis.
Methods
Rats were divided into 7 groups: normal control, SOF, SOF encapsulated in galactosylated taurocholate bilosomal formula (nano-SOF), galactosylated taurocholate bilosomal formula (nanoparticle), thioacetamide (TAA), TAA-SOF and TAA-nano-SOF. Liver fibrosis was induced by TAA (200 mg/kg) intraperitoneal injection twice per week for 8 weeks. SOF, nanoparticle and nano-SOF were given (40 mg/Kg/day) orally from day one of the study. Serum activities of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP) and tissue transforming growth factor beta (TGF-β) were assessed. Also, histopathological assessment of hepatic tissue was done.
Results
Administration of SOF and TAA to normal rats resulted in significant increase in serum AST, ALT, ALP and tissue TGF-β1 levels with variable degree of liver fibrosis. Additionally, rats in TAA group that received SOF therapy did not exhibit improved liver functions, TGF-β1 level and liver fibrosis score. However, administering nano-sofosbuvir prophylactically to TAA-treated rats resulted in a considerable improvement in liver function tests, TGF-1 levels, with liver fibrosis score regression.
Conclusion
In contrast to free sofosbuvir, SOF encapsulated in galactosylated taurocholate bilosomal formula (nano-SOF) displayed hepatoprotective effects in rat with thioacetamide-induced hepatic fibrosis. These findings strongly support the concept that galactoylatedbilosomes are promising nanocarrier for the targeted delivery of sofosbuvir to the liver.
期刊介绍：
Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.
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