rifampin and tyloxapol

Surface properties and aggregation behavior of cationic-cationic and cationic-non-ionic mixed surfactant systems viz. Dodecylethyldimethylammonium bromide (DDAB) with a series of double chain cationic surfactants (DiDDAB, DMDTAB, and DODAB) and non-ionic surfactants (Brij 96, Tyloxapol and Tween 80) were analysed using surface tension and transmission electron microscopy (TEM). The effect of chain length of cationic surfactant and hydrophilic-lypophilic balance (HLB) prominently observed in critical aggregation (cac) value. The aqueous solubility of anti-tuberculosis drug: rifampicin (RIF) was comparatively studied by UV-vis spectroscopy in presence of formulated micelles and vesicles. RIF was significantly solubilised in aqueous medium using all the formulated aggregates. RIF is very unstable in basic medium (above pH-7) and in oxidizing media. Therefore, stability at pH-13 as well as in strong oxidising environment was monitored using UV-vis spectroscopy. To trace the locus of the drug encapsulation in the micelles/vesicles, fluorescence spectroscopy and TEM studies were carried out. Both the techniques stemmed in complimentary results and confirmed that, RIF is majorly populated at polar medium in cationic-cationic vesicles and favour to reside at hydrophobic medium of the nonionic-cationic micelles.

Topics: Antitubercular Agents; Cations; Drug Carriers; Drug Liberation; Hydrophobic and Hydrophilic Interactions; Micelles; Nanoparticles; Plant Oils; Polyethylene Glycols; Polysorbates; Quaternary Ammonium Compounds; Rifampin; Solubility; Surface Properties; Surface Tension; Surface-Active Agents; Thermodynamics; Water

The present study delineates the formulation of niosomes from biocompatible surfactant Tyloxapol and their potential as drug delivery system for anti-tuberculosis drugs. Drug loaded niosomes have a size of 150 nm with a loading efficiency of 97.95±0.2, 98.89±0.2 and 99.50±0.2% for rifampicin (RIF), isoniazid (INH), pyrazinamide (PZA), respectively. Fourier transform infrared spectroscopic studies infer that the drugs are in harmony with the fabricated niosomes since no visible interactions between the drug and niosomes have been detected. The prepared formulations are quite stable as assessed using absorption spectroscopy. TEM images and photoluminescence results reveal that RIF and INH are located in the film bilayer whereas PZA is adsorbed mainly on the surface head groups. In vitro dissolution studies at physiological conditions have been undertaken to compare the release behavior of drugs from the prepared niosomes. Sustained release has been achieved for hydrophilic drugs and an acceptable release in case of RIF. Comparison of regression coefficients of different kinetic models reveal that INH release follows Fickian diffusion mechanism whereas RIF and PZA, a non-Fickian release mechanism. Such a versatile system is expected to reduce dose-related drug toxicity and reach the atelectatic areas.

Topics: Absorption; Antitubercular Agents; Chemistry, Pharmaceutical; Chromatography, High Pressure Liquid; Drug Compounding; Hydrogen-Ion Concentration; Isoniazid; Kinetics; Liposomes; Luminescence; Microscopy, Electron, Transmission; Particle Size; Polyethylene Glycols; Pyrazinamide; Pyrenes; Rifampin; Solubility; Spectroscopy, Fourier Transform Infrared; Surface-Active Agents

A non-ionic detergent, Triton WR-1339, prolonged markedly the survival time of mice infected fatally with virulent mycobacteria, though it exerted only a limited effect on the fate of tissue viable counts. The combined administration of Triton WR-1339 with lentinan (a glucan purified from the Japanese mushroom Lentinus edodes) was more effective than the single administration of each. This detergent was not lytic to red blood cells or lysosomes, but its substantial effect on the biomembrane was suggested by cold-shock experiment of hemolysis. It was considered that Triton WR-1339 is a biological-response modifier, possibly altering the interaction between the mycobacterial surface and the membrane structure of phagocytes.

Topics: Animals; Cell Membrane; Detergents; Drug Therapy, Combination; Lentinan; Lung; Male; Mice; Mycobacterium; Polyethylene Glycols; Pyrazinamide; Rifampin; Spleen; Tuberculosis