title: Cytotoxic evaluation of injectable cyclodextrin nanoparticles.
abstract: Nanoparticles were prepared using beta-CDC6, which is an amphiphilic beta-cyclodextrin derivative modified on the secondary face with 6C aliphatic esters. A nanoprecipitation technique was used to prepare the blank nanoparticles without any surfactant and nanoparticles containing Pluronic F68 as surfactant in a concentration range of 0.1 to 1%. Nanoparticle formulations were characterized by particle size distribution and zeta potential measurements. Entrapment efficiency and in-vitro release profiles were determined and the cytotoxicity of these injectable nanospheres was evaluated against mouse fibroblast L929 cell line and human polymorphonuclear cells by methlythiazolyltetrazolium assay. As far as particle size and zeta potential are concerned, there is a relationship between surfactant presence and nanoparticle characteristics. However, these effects are not significant. It was also found that surfactant presence has no effect on model drug nimodipine encapsulation but accelerates the in-vitro release of the drug. Cell culture studies on mouse fibroblasts and human polymorphonuclear cells revealed a concentration-dependent cytotoxicity more pronounced in fibroblast cells. This led to the conclusion that the use of surfactants in injectable nanoparticles prepared from amphiphilic beta-cyclodextrins may lead to altered in-vitro properties and impaired safety for the drug delivery system.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, 06100 Ankara, Turkey. eremino@hacettepe.edu.tr
authors.forename: Erem
authors.initials: E
authors.lastname: Memisoglu-Bilensoy
authors.forename: A Lale
authors.initials: AL
authors.lastname: Doğan
authors.forename: A Atilla
authors.initials: AA
authors.lastname: Hincal
mesh_terms: D000818:Animals; D002121:Calcium Channel Blockers / Q000737:chemistry; D002460:Cell Line; D002470:Cell Survival; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000737:chemistry; D004353:Drug Evaluation, Preclinical; D006801:Humans; D051379:Mice; D049329:Nanostructures; D009504:Neutrophils / Q000187:drug effects; D009553:Nimodipine / Q000737:chemistry; D020442:Poloxamer / Q000737:chemistry; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods; D047392:beta-Cyclodextrins / Q000737:chemistry / Q000633:toxicity*
chemical_list: D002121:Calcium Channel Blockers; D004337:Drug Carriers; D013501:Surface-Active Agents; D047392:beta-Cyclodextrins; D020442:Poloxamer; D009553:Nimodipine; C031215:betadex