Fluorinated and pegylated polyaspartamide derivatives toincrease solubility and efficacy of Flutamide

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Abstract

New fluorinated amphiphilic copolymers based on a biocompatible polyaspartamide have been prepared in orderto obtain polymeric micelles useful for delivering anticancer drugs. In particular, α,β-poly(N-2-hydroxyethyl)-d,laspartamide(PHEA) has been derivatized with polyethylene glycol (PEG2000) and ethylendiamine (EDA). Both theseportions form the hydrophilic part of the copolymer, while the hydrophobic moiety is given by 1,2,4-oxadiazoles:5-pentafluorophenyl-3-perfluoroheptyl-1,2,4-oxadiazole (PPOX) or 3-carboxyethyl-5-pentadecafluoroheptyl-1,2,4-oxadiazole (CPOX). Copolymers named PHEA-PEG2000-EDA-PPOX and PHEA-PEG2000-EDA-CPOX have been preparedwith various degrees of derivatization and characterized by spectroscopic analyses. Size exclusion chromatography,pyrene colorimetric assay, light scattering analysis and scanning electron microscopy have evidenced the occurrenceof a self-association process in aqueous medium. The ability of these aggregates to incorporate a hydrophobicdrug and increase its solubility has been evaluated by using Flutamide, a fluorinated anticancer agent. Moreover,the activity of Flutamide-loaded micelles on proliferation of dihydrotestosterone stimulated LNCaP cells has beendetermined and compared to that of free drug.
Lingua originaleEnglish
pagine (da-a)433-444
Numero di pagine12
RivistaJournal of Drug Targeting
Volume20
Stato di pubblicazionePublished - 2012

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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