Controlled dual activity of an organometallic antibiotic through micelle formulation

Abstract

Sodium Lauryl Sulphate (SLS) and Cetyltrimethylammonium bromide (CTAB) were employed to create micelles (SLS@CIPTIN and CTAB@CIPTIN) of the organometallic antibiotic Ph2Sn(CIP)2 (CIPTIN) (where HCIP= ciprofloxacin). The characterization of the micelles was conducted in the solid-state using melting point, Attenuated Total Reflectance-Fourier Transform Infra-Red (ATR-FTIR), 119Sn Mössbauer and X-ray Fluorescence (XRF) spectroscopies, and Thermogravimetry/Differential Thermal Analysis (TG-DTA), while in solution, by Ultra violet-Visible (UV–Vis) and Nucleus Magnetic Resonance (1HNMR ) spectroscopic techniques were employed. The compounds were tested for their antiproliferative activity against human breast adenocarcinoma cells: MCF-7 (hormone depended (HD)) and MDA-MB-231 (hormone independent (HI)). The in vitro and in vivo non-genotoxicity was confirmed with micronucleus (MN) and Artemia salina assay. The antiproliferative mechanism of action of SLS@CIPTIN and CTAB@CIPTIN was studied by cell morphology and cell cycle arrest. The antibacterial activity was evaluated using Minimum Inhibitory Concentration (MIC), Minimum Bactericidal Concentration (MBC) and Inhibition Zones (IZ) against Minimum Bactericidal Concentration (MBC) against Gram-negative strains P. aeruginosa, E. coli, as well as Gram-positive strains S. epidermidis and S. aureus. The results indicate that both the investigated CIPTIN and its supramolecular assembly (SLS@CIPTIN) exhibit activity. Therefore, the encapsulation of antimicrobial compounds can indeed be regarded as an attractive strategy for the development of new dual-active agents. These agents offer concurrent anticancer and antibacterial attributes without inducing toxicity.