Unilamellar vesicles as potential capreomycin sulfate carriers: Preparation and physicochemical characterization

Abstract

This increasing incidence of TB is attributable to several factors, the most important of which are the HIV epidemic and the lack of control of immigration from countries where TB is common. In fact, untreated HIV infection, leading to progressive immunodeficiency, increases susceptibility to TB, one of the main causes of death in populations with high HIV prevalence. 1-3The aim of this work was to evaluate unilamellar liposomes as new potential capreomycin sulfate (CS) delivery systems for future pulmonary targeting by aerosol administration. Dipalmitoylphosphatidylcholine, hydrogenated phosphatidylcholine, and distearoylphosphatidylcholine were used for liposome preparation. Peptide-membrane interaction was investigated by differential scanning calorimetry (DSC) and attenuated total internal reflection Fourier-transform infrared spectroscopy (ATIR-FTIR). Peptide entrapment, size, and morphology were evaluated by UV spectrophotometry, photocorrelation spectroscopy, and transmission electron microscopy, respectively. Interaction between CS and the outer region of the bilayer was revealed by DSC and ATIR-FTIR. DSPC liposomes showed enhanced interdigitation when the CS molar fraction was increased. Formation of a second phase on the bilayer surface was observed. From kinetic and permeability studies, CS loaded DSPC liposomes resulted more stable if compared to DPPC and HPC over the period of time investigated. The amount of entrapped peptide oscillated between 10% and 13%. Vesicles showed a narrow size distribution, from 138 to 166 nm, and a good morphology. These systems, in particular DSPC liposomes, could represent promising carriers for this peptide.

Nanomedicines as Drug Delivery Carriers of Anti-Tubercular Drugs: From Pathogenesis to Infection Control

“…They investigated that DSPC based liposome were found to be within narrow size distribution even less than 200 nm that offered suitability for inhalation formulation. Another authors explored that freeze thaw and surface response methodology was more effective and promising methodology to improve the drug content [53, 54]. Sparfloxacin (Flouroquinolone) was investigated for reduction in growth rate index using liposome loaded sparfloxacin.…”

Spray-Dried Powder Formulation of Capreomycin Designed for Inhaled Tuberculosis Therapy

“…In addition, dry powder inhalers (DPIs) are easy to operate and allow the delivery of high doses, which are often required for antibiotics [9]. A few studies have reported the preparation of inhalable powder of capreomycin, some of which were formulated in liposomes or poly(lactic-coglycolic acid) (PLGA) microparticles to control the particles size distribution for efficient lung deposition [10,11]. Hickey et al produced spray-dried powder of capreomycin (as sulfate), in which 50% ethanol (v/v) was used as the solvent and L-leucine as dispersion enhancer [2,[12][13][14].…”

Synthesis, characterization and in vitro extracellular and intracellular activity against Mycobacterium tuberculosis infection of new second-line antitubercular drug-palladium complexes

“…The efficient clearance of exogenous substances from the lungs complicates the successful development of suitable pulmonary anti‐TB drug delivery systems. Various approaches to this problem have been reported, such as the use of polymeric microparticles, large porous particles, liposomes and polymeric nanoparticles …”