81329-81-9Relevant articles and documents
Self-emulsifying drug delivery systems comprising chlorhexidine and alkyl-EDTA: A novel approach for augmented antimicrobial activity
Jalil, Aamir,Asim, Mulazim Hussain,Akkus, Zeynep Burcu,Schoenthaler, Martin,Matuszczak, Barbara,Bernkop-Schnürch, Andreas
, (2019)
The aim of the study was to develop a self-emulsifying drug delivery systems (SEDDS) comprising chlorhexidine (CX) and monododecylamide-EDTA (alkyl-EDTA) exhibiting enhanced microbicidal properties. SEDDS containing 20% Captex 300, 45% Cremophor EL, 17% Tween 80 and 18% DMSO were loaded with 3% (m/v) alkyl-EDTA (FA) and formulations of 1% CX and 1.5% (m/v) alkyl-EDTA (FA-CX1% and FA-ED1.5%) were prepared separately as well as in combination (FA-CX1%ED1.5%). Resazurin assay was performed to assess the biocompatibility of SEDDS in concentrations of 0.5% and 1%. Alkyl-EDTA SEDDS were also evaluated for their binding affinity towards Ca2+ and Mg2+ as well as for augmented antimicrobial properties using E. coli as model germ. Biocompatibility assay of SEDDS revealed that >85% of cells remained viable after 4 h. SEDDS FA efficiently bound 770 ± 19 μmol/g of calcium and 784 ± 16 μmol/g of magnesium, respectively. SEDDS FA-CX1%ED1.5% showed a 34.3- and 12.9-fold enhanced antimicrobial effect compared to FA-ED1.5% and FA-CX1%, respectively. The combination of CX with alkyl-EDTA in SEDDS seems therefore to be a promising strategy to enhance the antimicrobial activity of this antiseptic drug.
Synthesis, relaxivity, and T1 relaxation enhancement of binuclear gadolinium(III) complexes based on DTPA or EDTA and long-chain alkyl esters of L-lysine
Yu, Kaichao,Hamdan, Yousef,Wan, Fuxian,Li, Yinxia,Huang, Kaixun,Zhou, Jinlan
, p. 218 - 222 (2008/02/11)
Eight novel diamino-ester ligands were synthesized by amidation reaction of long-chain alkyl esters of l-lysine with diethylenetriamine pentaacetic acid monoanhydride or ethylenediamine tetraacetic acid monoanhydride. The corresponding dimeric Gd(iii) complexes were obtained by treating these ligands with GdCl3?6H2O. All ligands and complexes were characterized by 1H NMR, FT-IR, and elemental analysis. The longitudinal relaxation time (T1) was measured, and all relaxivity values (R1) of these dimeric Gd(iii) complexes are higher than that of Magnivest (Gd-DTPA). One of these complexes, possessing the highest relaxivity in the DTPA series, was chosen to test the acute toxicity and T 1-weighted imaging. It was found that this dimeric Gd(iii) complex exhibits no acute toxicity, and offers highly enhanced MRI signal and increases intention time in the rat liver tissue compared to Magnivest. CSIRO 2007.
Synthesis and characterization of cyclomaltoheptaose-based metal chelants as probes for intestinal permeability
Capretta,Maharajh,Bell
, p. 49 - 63 (2007/10/02)
The syntheses of two cyclomaltoheptaose-based metal chelants, cyclomaltoheptaose-ethylenediaminetetraacetate (CD-EDTA) and cyclomaltoheptaose-diamide-disulfur (CD-DADS), are described. The chelant moieties are attached to the 6-position of a single pyranose in the cyclomaltoheptaose via a short diamine spacer chain. Characterization of these novel chelants has been achieved using NMR and MS techniques. The peculiar fluxional properties of the CD-EDTA molecules is also discussed.