title: Laminin receptor-targeted etoposide loaded polymeric micelles: a novel approach for the effective treatment of tumor metastasis.
abstract: BACKGROUND
  Tumor-targeted delivery is a desirable approach to improve therapeutic outcome of anticancer drug due to enhanced efficacy and reduced toxicity.
  
  
  OBJECTIVE
  The present study was aimed to target laminin receptor over-expressed tumor cells using YIGSR (Tyr-Ile-Gly-Ser-Arg) conjugated etoposide loaded micelles in the treatment of metastasis.
  
  
  METHODS
  YIGSR conjugated micelles prepared using synthesized carboxyl and methoxy terminated poly(ethylene glycol)-b-poly(ϵ-caprolactone) block copolymers were evaluated for it efficacy against highly metastatic B16F10 cell lines conducting cytotoxicity, colony formation, cell migration, cellular uptake and flow cytometry studies. The in-vivo antimetastatic effect of micelles was evaluated using experimental metastatic model on C57BL/6 mice.
  
  
  RESULTS
  YIGSR conjugated micelles of particle size 45.2±3.77 nm and zeta potential of-5.7±1.3 mV demonstrated enhanced cytotoxicity and cellular uptake with significant reduction in colony formation and cell migration activities compared to non-conjugated micelles. Furthermore, a markedly inhibition in lung colony formation was observed with these micelles.
  
  
  CONCLUSIONS
  An enhanced cellular internalization of YIGSR conjugated micelles due to laminin receptor based endocytosis resulted in to higher cytotoxicity as well as antimetastatic effect against highly metastatic B16F10 cells.
  
  
  CONCLUSIONS
  These studies indicate that YIGSR conjugated nanocarrier can be a promising approach in the treatment of tumor metastasis.
authors.affiliation: Centre for Post Graduate Studies and Research, New Drug Delivery Systems Laboratory, Pharmacy Department, The M. S. University of Baroda, Vadodara, India.
authors.forename: Mukesh
authors.initials: M
authors.lastname: Ukawala
authors.forename: Kiran
authors.initials: K
authors.lastname: Chaudhari
authors.forename: Tushar
authors.initials: T
authors.lastname: Rajyaguru
authors.forename: A S
authors.initials: AS
authors.lastname: Manjappa
authors.forename: R S R
authors.initials: RS
authors.lastname: Murthy
authors.forename: Rajiv
authors.initials: R
authors.lastname: Gude
mesh_terms: D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods*; D005047:Etoposide / Q000008:administration & dosage* / Q000378:metabolism; D005260:Female; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000556:secondary*; D008546:Melanoma, Experimental / Q000188:drug therapy / Q000378:metabolism / Q000556:secondary; D051379:Mice; D008810:Mice, Inbred C57BL; D008823:Micelles; D011108:Polymers / Q000008:administration & dosage* / Q000378:metabolism; D011897:Random Allocation; D017474:Receptors, Laminin / Q000378:metabolism; D016896:Treatment Outcome
chemical_list: D008823:Micelles; D011108:Polymers; D017474:Receptors, Laminin; D005047:Etoposide