title: Curcumin-polymeric nanoparticles against colon-26 tumor-bearing mice: cytotoxicity, pharmacokinetic and anticancer efficacy studies.
abstract: BACKGROUND
  Curcumin (CUR), can inhibit proliferation and induce apoptosis of tumor cells, its extreme insolubility and limited bioavailability restricted its clinical application.
  
  
  OBJECTIVE
  An innovative polymeric nanoparticle of CUR has been developed to enhance the bioavailability and anti-cancer efficacy of CUR, in vitro and in vivo.
  
  
  METHODS
  Cationic copolymer Eudragit E 100 was selected as carrier, which can enhance properties of poor bioavailable chemotherapeutic drugs (CUR). The CUR-loaded Eudragit E 100 nanoparticles (CENPs) were prepared by emulsification-diffusion-evaporation method. The in vitro cytotoxicity study of CENPs was carried out using sulphorhodamine B assay. Pharmacokinetic and anti-cancer efficacy of CENPs was investigated in Wister rats as well as colon-26 tumor-bearing mice after oral administration.
  
  
  RESULTS
  CENPs showed acceptable particle size and percent entrapment efficiency. In vitro cytotoxicity studies in terms of 50% cell growth inhibition values demonstrated ∼19-fold reduction when treated with CENPs as compared to pure CUR. ∼91-fold increase in Cmax and ∼95-fold increase in AUC0-12h were observed indicating a significant enhancement in the oral bioavailability of CUR when orally administered as CENPs compared to pure CUR. The in vivo anti-cancer study performed with CENPs showed a significant increase in efficacy compared with pure CUR, as observed by tumor volume, body weight and survival rate.
  
  
  CONCLUSIONS
  The results clearly indicate that the developed polymeric nanoparticles offer a great potential to improve bioavailability and anticancer efficacy of hydrophobic chemotherapeutic drug.
authors.affiliation: a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University) , Varanasi , Uttar Pradesh , India.
authors.forename: Sundeep
authors.initials: S
authors.lastname: Chaurasia
authors.affiliation: a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University) , Varanasi , Uttar Pradesh , India.
authors.forename: Pramila
authors.initials: P
authors.lastname: Chaubey
authors.affiliation: a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University) , Varanasi , Uttar Pradesh , India.
authors.forename: Ravi R
authors.initials: RR
authors.lastname: Patel
authors.affiliation: a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University) , Varanasi , Uttar Pradesh , India.
authors.forename: Nagendra
authors.initials: N
authors.lastname: Kumar
authors.affiliation: a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University) , Varanasi , Uttar Pradesh , India.
authors.forename: Brahmeshwar
authors.initials: B
authors.lastname: Mishra
mesh_terms: D000179:Acrylates / Q000737:chemistry; D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001682:Biological Availability; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003106:Colon / Q000187:drug effects / Q000378:metabolism; D003110:Colonic Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D003474:Curcumin / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D004337:Drug Carriers / Q000737:chemistry; D005260:Female; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D011108:Polymers / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility
chemical_list: D000179:Acrylates; D000970:Antineoplastic Agents; D004337:Drug Carriers; C477020:Eudragit E100; D011108:Polymers; D003474:Curcumin
keywords: Anti-cancer efficacy; bioavailability; colon-26 cells; cytotoxicity; polymeric nanoparticles