title: [Formulation and characetization of self-microemulsifying drug delivery systems according to their cytotoxic attributes].
abstract: The aim of this study was to develop and examine novel drug delivery systems upon the cytotoxic behaviour of their tenside components. Different self-emulsifying combinations have been formulated by water dilution and oil dilution method with various previously tested tensides and co-tensides. The visual properties registered against the increment of the applied tenside component in Ternary triangular diagrams. Cartesian coordinate calculation was applied to select the adequate compositions. Self-emulsifying drug delivery systems are wildly used for enhanced bioavailabilty of oraly administrated pharmacons. Full particulars of topical application of these systems have not been evaluated yet. In our study the cellular effects of the applied amphiphilic tensides on human Caco-2 and HeLa cell monolayers as dependent upon their chemical structures and physicochemical properties have been evaluated. Cytotoxicity investigation was performed on Caco-2 and HeLa cells by MTT method. HeLa cells as in vitro model of cervix and Caco-2 cell monolayers as convenient and reliable in vitro models of the gastrointestinal tract have been chosen. According to the results of the formulation procedures it can be determined that each developed SMEDD mixtures belong to type IIIa or IIIb in the lipid formulation classification system (LFCS) proposed by Pouton. All of the formulated systems were immediately emulsified within the first second of contact with distilled water as dispersion medium and no evidence of phase separation or any instability problem have been observed for at least 72 h. The droplet diameter of dispersed self emulsifying compositions has been evaluated by Dynamic Light Scattering device. We concluded that the increased Transcutol HP concentrations lead to an obvious improvement in the optical clarity, which correlates with the determined particle size of the corresponding dispersion. In cytotoxicity test the toxic properties of the applied tensides have not been found as additive parameter. The most toxic component determined the cytotoxicitxy of the SMEDDS. Our results might ensure useful data for formulation of suitable SMEDDS with lower active ingredient necessity. Developed SMEDDS might be advantageous in terms of increased bioavailability, minimized side effect, and hence the patient compliance.
authors.forename: Zoltán
authors.initials: Z
authors.lastname: Ujhelyi
authors.forename: Miklós
authors.initials: M
authors.lastname: Vecsernyés
authors.forename: Ildikó
authors.initials: I
authors.lastname: Bácskay
mesh_terms: D001682:Biological Availability; D018938:Caco-2 Cells; D002470:Cell Survival / Q000187:drug effects*; D002584:Cervix Uteri / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D003603:Cytotoxins / Q000494:pharmacology*; D016503:Drug Delivery Systems / Q000379:methods*; D004655:Emulsions; D005260:Female; D041981:Gastrointestinal Tract / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans
chemical_list: D003603:Cytotoxins; D004655:Emulsions