Formulation and evaluation of rutin-loaded solid lipid nanoparticles for the treatment of brain tumor
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ORIGINAL ARTICLE
Formulation and evaluation of rutin-loaded solid lipid nanoparticles for the treatment of brain tumor Sureshbabu Ram Kumar Pandian 1 & Parasuraman Pavadai 2 & Sivakumar Vellaisamy 3 & Vigneshwaran Ravishankar 4 & Ponnusamy Palanisamy 5 & Lakshmi M. Sundar 2 & Vivek Chandramohan 6 & Murugesan Sankaranarayanan 7 & Theivendren Panneerselvam 8 & Selvaraj Kunjiappan 1 Received: 13 August 2020 / Accepted: 29 October 2020 # Springer-Verlag GmbH Germany, part of Springer Nature 2020
Abstract The primary requirement for curing cancer is the delivery of essential drug load at the cancer microenvironment with therapeutic efficacy. Considering this, the present study aims to formulate “Rutin”-encapsulated solid lipid nanoparticles (SLNs) for effective brain delivery across the blood-brain barrier (BBB). Rutin-loaded SLNs were fabricated by oil-in-water microemulsion technique and were characterized for their physicochemical properties. The in vivo biodistribution study of rutin-loaded SLNs was studied using Rattus norvegicus rats. Subsequently, in silico molecular docking and dynamic calculations were performed to examine the binding affinity as well as stability of rutin at the active site of target protein “epidermal growth factor receptor (EGFR).” Formulated rutin-loaded SLNs were predominantly spherical in shape with an average particle diameter of 100 nm. Additionally, the biocompatibility and stability have been proved in vitro. The presence and biodistribution of rutin in vivo after 54 h of injection were observed as 15.23 ± 0.32% in the brain, 8.68 ± 0.63% in the heart, 4.78 ± 0.28% in the kidney, 5.04 ± 0.37% in the liver, 0.92 ± 0.04% in the lung, and 11.52 ± 0.65% in the spleen, respectively. Molecular docking results revealed the higher binding energy of − 150.973 kJ/mol of rutin with EGFR. Molecular dynamic simulation studies demonstrated that rutin with EGFR receptor complex was highly stable at 30 ns. The observed results exemplified that the formulated rutin-loaded SLNs were stable in circulation for a period up to 5 days. Thus, rutin-encapsulated SLN formulations can be used as a promising vector to target tumors across BBB.
Keywords Biodistribution . Targeted delivery . Epidermal growth factor . Molecular docking . Molecular dynamics . Microemulsion
Supplementary Information The online version contains supplementary material available at https://doi.org/10.1007/s00210-02002015-9. * Murugesan Sankaranarayanan [email protected] * Theivendren Panneerselvam [email protected] * Selvaraj Kunjiappan [email protected]
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Department of Biotechnology, Mepco Schlenk Engineering College, Sivakasi, Tamilnadu 626005, India
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School of Mechanical Engineering, Vellore Institute of Technology, Vellore, Tamilnadu 632014, India
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Department of Biotechnology, Siddaganga Institute of Technology, Tumakuru, Karnataka 572103, India
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Department of Biotechnology, Kalasalingam Academy of Research and Education, Krishnankoil, Tamilnadu 626126, India
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Department of Pharmaceutical Chem
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