title: Entrapment of 5-fluorouracil into PLGA matrices using supercritical antisolvent processes.
abstract: OBJECTIVE
  Two different supercritical antisolvent processes were performed to co-precipitate 5-fluorouracil (5-FU) and poly(lactide-co-glycolide) simultaneously. 5-FU is a hydrophilic antitumor agent, and is more effective when administered at a lower dose for a longer period of time.
  
  
  METHODS
  Controlled-release polymeric systems of 5-FU were produced, and morphology, thermal behavior, in-vitro release and cytotoxicity of microparticles were analysed.
  
  
  RESULTS
  Dissolution studies showed that 33% of drug was released in 21 days, which represents a long-lasting profile. To evaluate the efficacy of the released drug on cancer cells, the MTT assay cytotoxicity test was performed using human lung carcinoma A549 cell lines. There was no significant difference between the cell inhibition rates of the released drug and unprocessed 5-FU at the same drug concentration level. IC50 values were 69.12 mg/ml for unprocessed 5-FU and 68.71 mg/ml for the released drug.
  
  
  CONCLUSIONS
  Application of supercritical processing for co-precipitation of 5-FU and PLGA provided mild and non-aqueous conditions, so the hydrophilic drug incorporated in the polymer had good stability during the process.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences National Cell Bank of Iran, Pasteur Institute of Iran, Tehran, Iran.
authors.forename: Pardis
authors.initials: P
authors.lastname: Kalantarian
authors.forename: Ismaeil
authors.initials: I
authors.lastname: Haririan
authors.forename: Abdolhossein Rouholamini
authors.initials: AR
authors.lastname: Najafabadi
authors.forename: Mohammad Ali
authors.initials: MA
authors.lastname: Shokrgozar
authors.forename: Alireza
authors.initials: A
authors.lastname: Vatanara
mesh_terms: D045744:Cell Line, Tumor; D011232:Chemical Precipitation; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D004355:Drug Stability; D005472:Fluorouracil / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000633:toxicity; D006801:Humans; D011098:Polyglactin 910 / Q000737:chemistry / Q000633:toxicity; D012995:Solubility
chemical_list: D003692:Delayed-Action Preparations; D011098:Polyglactin 910; D005472:Fluorouracil