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Capecitabine lipid nanoparticles for anti-colon cancer activity in 1,2-dimethylhydrazine-induced colon cancer: preparation,cytotoxic, pharmacokinetic,and pathological evaluation
Authors:Narendar Dudhipala  Goverdhan Puchchakayala
Affiliation:1. Department of Pharmaceutics, Vaagdevi Pharmacy College, Warangal, India;2. Department of Pharmacology, Synapse Life Sciences, Vaagdevi College of Pharmacy, Hanmakonda, Warangal, India
Abstract:The cornerstone of this investigation is to determine the pharmacokinetic and histopathological behavior of solid lipid nanoparticles of capecitabine (CB-SLNs) in 1,2-dimethylhydrazine (DMH) induced colon cancer. The nanoparticles were prepared by microemulsion method. CB-SLNs were characterized for an optimal system. The cytotoxicity of CB-SLNs was evaluated by using MTT assay method. Further, pharmacokinetic and histopathological behavior of SLNs were studied in DMH induced colon cancer rats. The optimized nanoparticles have the particle size, zeta potential, and entrapment efficiency of 145.6?±?3.6?nm, ?26.9?±?2.7?mV, and 88.33?±?3.74%, respectively. Particles of CB were nearly spherical in shape and converted to amorphous form revealed by SEM and DSC, XRD studies. The nanoparticles showed dose-dependent cytotoxicity activity from 10 to 125?µg/mL compared with suspension. Pharmacokinetic studies revealed that 2.7-folds enhancement in the oral bioavailability and in aberrant crypt foci number, apoptotic index comparison with suspension formulation.
Keywords:Capecitabine  lipid nanoparticles  1  2-dimethylhydrazine  colon cancer  aberrant crypt foci  pharmacokinetics  histopathology
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