Preeti Pandey1, Mahfoozur Rahman2, Prakash Chandra Bhatt3, Sarwar Beg4, Basudev Paul4, Abdul Hafeez5, Fahad A Al-Abbasi6, Muhammad Shahid Nadeem7, Othman Baothman7, Firoz Anwar6,7, Vikas Kumar1. 1. Natural Product Drug Discovery Laboratory, Department of Pharmaceutical Sciences, Faculty of Health Sciences, Sam Higginbottom University of Agriculture, Technology & Sciences, Allahabad-211007, UP, India. 2. Department of Pharmaceutical Sciences, Shalom Institute of Health & Allied Sciences, Sam Higginbottom University of Agriculture, Technology & Sciences, Allahabad-211007, UP, India. 3. Centre for Advanced Research in Pharmaceutical Sciences, Microbial & Pharmaceutical Biotechnology Laboratory, Faculty of Pharmacy, Jamia Hamdard, New Delhi-110062, India. 4. Product Development Research, Jubilant Generics Limited, Noida-201301, UP, India. 5. Glocal School of Pharmacy, Glocal University, Saharanpur, UP, India. 6. Department of Biochemistry, Cancer Metabolism & Epigenetic Unit, Faculty of Science, Center of Innovation in Personalized Medicine, Cancer & Mutagenesis Unit, King Fahd Center for Medical Research, King Abdulaziz University, Jeddah, Saudi Arabia. 7. Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.
Abstract
AIM: The present work describes the development of poly(lactic co-glycolic acid) (PLGA) nanoparticles (NPs) of rutin (RT) for the treatment of hepatocellular carcinoma in rats. MATERIALS & METHODS: RT-loaded PLGA NPs (RT-PLGA-NPs) were prepared by double emulsion evaporation method. Further these are optimized by Box-Behnken design. PLGA NPs were evaluated for size, polydispersity index, drug-loading capacity, entrapment, gastric stability, in vitro drug release, in vivo preclinical studies and biochemical studies. RESULTS: Preclinical evaluation of RT-PLGA-NPs for anticancer activity through oral route exhibited significant improvement in hepatic, hematologic and renal biochemical parameters. Highly superior activity was observed in regulating oxidative stress and inflammatory markers, antioxidant enzymes, cytokines and inflammatory mediators and their role on plasma membrane ATPases responsible for destruction in liver tissues. CONCLUSION: Histopathological evaluation indicated reduced incidence of hepatic nodules, necrosis formation, infiltration of inflammatory cells, blood vessel inflammation and cell swelling with RT-PLGA-NP treatment along with considerable downregulation in the levels of proinflammatory cytokines.
AIM: The present work describes the development of poly(lactic co-glycolic acid) (PLGA) nanoparticles (NPs) of rutin (RT) for the treatment of hepatocellular carcinoma in rats. MATERIALS & METHODS: RT-loaded PLGA NPs (RT-PLGA-NPs) were prepared by double emulsion evaporation method. Further these are optimized by Box-Behnken design. PLGA NPs were evaluated for size, polydispersity index, drug-loading capacity, entrapment, gastric stability, in vitro drug release, in vivo preclinical studies and biochemical studies. RESULTS: Preclinical evaluation of RT-PLGA-NPs for anticancer activity through oral route exhibited significant improvement in hepatic, hematologic and renal biochemical parameters. Highly superior activity was observed in regulating oxidative stress and inflammatory markers, antioxidant enzymes, cytokines and inflammatory mediators and their role on plasma membrane ATPases responsible for destruction in liver tissues. CONCLUSION: Histopathological evaluation indicated reduced incidence of hepatic nodules, necrosis formation, infiltration of inflammatory cells, blood vessel inflammation and cell swelling with RT-PLGA-NP treatment along with considerable downregulation in the levels of proinflammatory cytokines.
Authors: Sarwar Beg; Ankit K Malik; Mohammad Javed Ansari; Asrar A Malik; Ahmed Mahmoud Abdelhaleem Ali; Abdulrahman Theyab; Mohammad Algahtani; Waleed H Almalki; Khalid S Alharbi; Sattam K Alenezi; Md Abul Barkat; Mahfoozur Rahman; Hani Choudhry Journal: ACS Omega Date: 2022-05-10