title: Cell Line and Augument Cellular Uptake Study of Statistically Optimized Sustained Release Capecitabine Loaded Eudragit S100/PLGA(poly(lacticco- glycolic acid)) Nanoparticles for Colon Targeting.
abstract: BACKGROUND
  Capecitabine, an anti cancer drug, has a very short drug elimination half-life (0.49 to 0.89 h). High doses and absence of targeting ability in the colon region may lead to more side effects to the patients with colon cancer.
  
  
  OBJECTIVE
  To develop and optimize sustained release nanoparticles for effective treatment of colon cancer.
  
  
  METHODS
  Eudragit S100-PLGA(poly (lactic-co-glycolic acid)) nanoparticles were prepared by a double emulsification, solvent evaporation method followed by high-pressure homogenisation evaluated and the particles were evaluated for surface morphology, particle size analysis, polydispersity index, drug content, % entrapment efficiency and in vitro drug release. To optimize the batch a 32 full factorial design was applied. The optimized batch was evaluated for cytotoxicity and cellular uptake study.
  
  
  CONCLUSIONS
  The optimized formulation exhibited 179.25 nm mean particle size, 71.27% of drug entrapment efficiency and 81.824% drug release up to 72 h. When the concentration of capecitabine was increased from 50-500 μg/ml, the % cytotoxicity of nanoparticles and capecitabine (pure drug) increased from 8.5 to 97.70% and 2.7 to 82.23%, respectively. As per a cellular uptake study, the optimized nanoparticles were completely uptaken by HT 29 adenocarcinoma cells within 2 to 4 h.
  
  
  CONCLUSIONS
  Optimized Eudragit S100-PLGA nanoparticles are a promising delivery system for colon targeting.
authors.affiliation: Maliba Pharmacy College, Uka Tarsadia University, Bardoli, Gujarat, India.
authors.forename: Sonia
authors.initials: S
authors.lastname: Pandey
authors.affiliation: Bhagwan Mahavir College of Pharmacy, Surat, Gujarat, India.
authors.forename: Sanganala Mattha
authors.initials: SM
authors.lastname: Vijayendra Swamy
authors.affiliation: C.L. Baid Metha College of Pharmacy, Chennai, India.
authors.forename: Udhshu Mansha
authors.initials: UM
authors.lastname: Ubaid Ulla
authors.affiliation: Maliba Pharmacy College, Uka Tarsadia University, Bardoli, Gujarat, India.
authors.forename: Arti
authors.initials: A
authors.lastname: Gupta
authors.affiliation: Maliba Pharmacy College, Uka Tarsadia University, Bardoli, Gujarat, India.
authors.forename: Hetal
authors.initials: H
authors.lastname: Patel
authors.affiliation: Vidya Bharati Trust College of Pharmacy, Umarakh, Bardoli, Gujarat, India.
authors.forename: Jitendra Singh
authors.initials: JS
authors.lastname: Yadav
mesh_terms: D000069287:Capecitabine / Q000008:administration & dosage* / Q000737:chemistry*; D002460:Cell Line; D045744:Cell Line, Tumor; D003106:Colon / Q000187:drug effects*; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D065546:Drug Liberation / Q000187:drug effects; D019073:HT29 Cells; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011109:Polymethacrylic Acids / Q000737:chemistry; D012997:Solvents / Q000737:chemistry
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011109:Polymethacrylic Acids; D012997:Solvents; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; C038300:methylmethacrylate-methacrylic acid copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000069287:Capecitabine
keywords: Cytotoxicity; capecitabine; controlled release; factorial design; nanoparticles; targeting