title: Effect of surface capping on targeting potential of folate decorated poly (propylene imine) dendrimers.
abstract: OBJECTIVE
  The objective of the present investigation was to assess and compare the effect of surface capping by different groups (-OH, -COOH and -NH2) on tumor targeting potential of folate conjugated poly (propylene imine) (PPI) (F-PPI) dendrimers using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay.
  
  
  METHODS
  The synthesized nanoconjugates (F-PPI, F-COOH-PPI, F-OH-PPI and F-CONH-PPI) were characterized by Fourier transform infrared spectroscopy (FT-IR), nuclear magnetic resonance ((1)H-NMR) and transmission electron microscopic (TEM) studies. The formulations were evaluated for drug entrapment, in vitro drug release and hemolytic toxicity, and cytotoxicity was evaluated on HeLa and SiHa cell line using MTT assay.
  
  
  RESULTS
  In case of all surface capped formulation, Methotrexate (MTX) loading was found to increased; however MTX release rate was found to decrease as compared to unmodified formulation. Further, F-COOH-PPI displayed highest tumor targeting potential as compared to other formulations. This is the first study to explore the effect of surface capping on the targeting potential of folate-conjugated fifth generation (5.0 G) PPI dendrimer.
  
  
  CONCLUSIONS
  In conclusion, the targeting potential of all the formulations (anticancer activity) for both HeLa and SiHa cells follows in the following order: F-COOH-PPI > F-OH-PPI > F-CONH-PPI > F-PPI.
authors.affiliation: Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, School of Engineering and Technology, Dr. Hari Singh Gour University , Sagar , India.
authors.forename: Babulal
authors.initials: B
authors.lastname: Birdhariya
authors.forename: Prashant
authors.initials: P
authors.lastname: Kesharwani
authors.forename: Narendra Kumar
authors.initials: NK
authors.lastname: Jain
mesh_terms: D050091:Dendrimers / Q000008:administration & dosage / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods; D005492:Folic Acid / Q000008:administration & dosage / Q000737:chemistry*; D006367:HeLa Cells; D006461:Hemolysis / Q000187:drug effects / Q000502:physiology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D046529:Microscopy, Electron, Transmission; D011126:Polypropylenes / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D050091:Dendrimers; D011126:Polypropylenes; C443641:poly(propyleneimine); D005492:Folic Acid
keywords: Cancer; cytotoxicity; dendrimers; folate; methotrexate