title: Modified dipeptide-based nanoparticles: vehicles for targeted tumor drug delivery.
abstract: OBJECTIVE
  Different nanoparticles have been investigated to deliver chemotherapeutic agents, but complex synthesis procedures and biocompatibility issues raise concerns in developing them for safe human usage. The aim of this work is to develop α,β-dehydrophenylalanine-containing, self-assembled, amphipathic dipeptide nanoparticles for tumor-targeted drug delivery and therapy.
  
  
  METHODS
  Solution-phase peptide synthesis was used to synthesize dipeptides. Nanoparticles were prepared by molecular self-assembly. A tumor distribution study was carried out using a radiolabeling method. Tumor regression studies were carried out in murine ascitic tumors in BALB/c mice and breast tumor xenografts in in nonobese diabetic/severe combined immunodeficiency mice.
  
  
  RESULTS
  Arg-α,β-dehydrophenylalanine formed self-assembled nanoparticles that could be easily derivatized with folic acid. Folic acid-derivatized nanoparticles showed enhanced cellular uptake and, when loaded with doxorubicin, showed enhanced tumor regression compared with underivatized nanoparticles or native drug, without any adverse side effects, both in vitro and in vivo.
authors: International Centre for Genetic Engineering & Biotechnology, New Delhi 110067, India.
authors: Jiban J
authors: JJ
authors: Panda
authors: Ankur
authors: A
authors: Kaul
authors: Santosh
authors: S
authors: Kumar
authors: Shadab
authors: S
authors: Alam
authors: Anil K
authors: AK
authors: Mishra
authors: Gopal C
authors: GC
authors: Kundu
authors: Virander S
authors: VS
authors: Chauhan
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D045744:Cell Line, Tumor; D004151:Dipeptides / Q000737:chemistry* / Q000378:metabolism; D004317:Doxorubicin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D005260:Female; D005492:Folic Acid / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000737:chemistry* / Q000378:metabolism; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D010649:Phenylalanine / Q000031:analogs & derivatives / Q000378:metabolism
chemical_list: D000903:Antibiotics, Antineoplastic; D004151:Dipeptides; D010649:Phenylalanine; D004317:Doxorubicin; D005492:Folic Acid