title: Novel microspheres based on triterpene saponins from the roots of Physospermum verticillatum (Waldst & Kit) (Apiaceae) for the improvement of gemcitabine release.
abstract: OBJECTIVE
  This study concerns the preparation and characterization of microspheres based on a mixture of triterpene saponins, from Physospermum verticillatum (Waldst & Kit), as a carrier for the specific release of gemcitabine.
  
  
  METHODS
  Triterpene saponins were derivatized with acrylic acid. The obtained polymerizable product was characterized by Fourier transform infrared to confirm the ester linkage. Then, spherical microparticles were prepared by suspension radical copolymerization and impregnated with gemcitabine.
  
  
  RESULTS
  Microspheres exhibited a mean diameter of 2.7 μ. The swelling studies showed that particles swell most at pH 6.2, typical of the tumour pathology, than at pH 7.4, miming physiological conditions. The microspheres were loaded with gemcitabine (LE 72.2%). Their release profile showed an initial dot of around 24% and a further release for 24 h.
  
  
  CONCLUSIONS
  This carrier could be potentially release the drug in the lung, as a function of different pHs between tumour cells and healthy, reducing the systemic drug toxicity, allowing the reduction of the doses number, increasing the drug half-life and eliminating the problems related to the fast clearance of gemcitabine administration.
authors.affiliation: Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata di Rende, Cosenza, Italy.
authors.forename: Sonia
authors.initials: S
authors.lastname: Trombino
authors.affiliation: Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata di Rende, Cosenza, Italy.
authors.forename: Roberta
authors.initials: R
authors.lastname: Cassano
authors.affiliation: Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata di Rende, Cosenza, Italy.
authors.forename: Silvia
authors.initials: S
authors.lastname: Mellace
authors.affiliation: Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata di Rende, Cosenza, Italy.
authors.forename: Nevio
authors.initials: N
authors.lastname: Picci
authors.affiliation: Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata di Rende, Cosenza, Italy.
authors.forename: Monica R
authors.initials: MR
authors.lastname: Loizzo
authors.affiliation: Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata di Rende, Cosenza, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Menichini
authors.affiliation: Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata di Rende, Cosenza, Italy.
authors.forename: Rosa
authors.initials: R
authors.lastname: Tundis
mesh_terms: D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000737:chemistry; D019661:Apiaceae / Q000737:chemistry*; D003841:Deoxycytidine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry* / Q000302:isolation & purification; D004339:Drug Compounding; D065546:Drug Liberation; D006863:Hydrogen-Ion Concentration; D008863:Microspheres; D018517:Plant Roots / Q000737:chemistry*; D012503:Saponins / Q000737:chemistry* / Q000302:isolation & purification; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D014315:Triterpenes / Q000737:chemistry* / Q000302:isolation & purification; D000093542:Gemcitabine
chemical_list: D000964:Antimetabolites, Antineoplastic; D004337:Drug Carriers; D012503:Saponins; D014315:Triterpenes; D003841:Deoxycytidine; D000093542:Gemcitabine
keywords: gemcitabine; lung cancer; microspheres; release; triterpene saponins