title: Role of the pharmaceutical excipients in the tamoxifen activity on MCF-7 and vero cell cultures.
abstract: BACKGROUND
  Microparticles are used for controlled drug delivery. With the aim of improving both bioavailability and tamoxifen selective toxicity, the activity of tamoxifen embedded in calcium alginate/chitosan microparticles was studied.
  
  
  METHODS
  Tamoxifen alone and embedded in microparticles prepared with sodium alginate from Kelco (62% mannuronic acid and 38% guluronic acid) and from Fluka (30% mannuronic acid and 70% guluronic acid) was added to MCF-7 and Vero cultures and evaluated for antiproliferative activity by the MTT test.
  
  
  RESULTS
  The use of Kelco or Fluka alginate resulted in different LD(50) values on Vero and MCF-7 cultures, showing a higher cytotoxicity toward Vero cells treated with tamoxifen embedded in Kelco microparticles (25 microM vs. 48 microM on MCF-7 cells) but a selective toxicity with Fluka microparticles (25 microM and 10 microM on Vero and MCF-7 cells respectively).
  
  
  CONCLUSIONS
  Microparticle formulation may improve selective toxicity according to the alginate employed: differences in the chemical alginate composition can dramatically change both drug activity and toxicity.
authors.affiliation: Department of Biomedical Sciences, University of Modena and Reggio Emilia, Via G. Campi 287, 41100 Modena Italy. tiziana.rossi@unimore.it
authors.forename: Tiziana
authors.initials: T
authors.lastname: Rossi
authors.forename: Valentina
authors.initials: V
authors.lastname: Iannuccelli
authors.forename: Gilberto
authors.initials: G
authors.lastname: Coppi
authors.forename: Elisa
authors.initials: E
authors.lastname: Bruni
authors.forename: Giosué
authors.initials: G
authors.lastname: Baggio
mesh_terms: D000464:Alginates / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D048708:Cell Growth Processes / Q000187:drug effects; D045744:Cell Line, Tumor; D048271:Chitosan / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D005079:Excipients / Q000737:chemistry / Q000494:pharmacology*; D020723:Glucuronic Acid / Q000737:chemistry / Q000494:pharmacology; D006603:Hexuronic Acids / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D010316:Particle Size; D013629:Tamoxifen / Q000737:chemistry / Q000494:pharmacology*; D014709:Vero Cells
chemical_list: D000464:Alginates; D005079:Excipients; D006603:Hexuronic Acids; D013629:Tamoxifen; D020723:Glucuronic Acid; D048271:Chitosan