Studying the activity of antitubercluosis drugs inside electrospun polyvinyl alcohol, polyethylene oxide, and polycaprolacton nanofibers

Abstract

The activity of antituberculosis drugs (streptomycin sulfate, isoniazid, pyrazinamid, and clarithromycin) embedded in biodegradable nanofibers against Mycobacterium avium has been studied by broth dilution assay and by agar plate assay. These drugs have also been embedded in electrospun polyvinyl alcohol (PVA), polyethylene oxide (PEO), and polycaprolacton (PCL) nanofibers to design a new single tablet containing first-line antituberculosis drugs. Our results show that antituberculosis drugs are active at tiny amounts (up to 300 µg mL(-1) of solvent). However, within polymer matrices, high amounts of drugs are required to avoid unwanted weak interactions within PEO and PCL matrices. The successful design of a single tablet containing required amounts of antituberculosis drugs is essential for the full treatment of tuberculosis in patients with HIV.

Interactions between Chloramphenicol, Carrier Polymers, and Bacteria–Implications for Designing Electrospun Drug Delivery Systems Countering Wound Infection

“…Altogether, our data indicate that the complex interplay between the nature of the drug, drug release kinetics and carrier polymer properties determine the effectiveness of antimicrobial therapy. Interactions between drug molecules and carrier polymers can have a detrimental effect on antibacterial activity, as was shown by Hassounah et al demonstrating that hydrogen bonding between polyvinylpyrrolidone (PVP) carrier and antituberculosis drugs resulted in the loss of antibacterial activity . It seems that most beneficial release profile would be initial burst release to quickly reach effective antibacterial concentrations together with more prolonged release to keep the concentrations sufficient for longer time and prevent biofilm formation on the dressing and in the wound.…”

Nanopartículas como transportadores de fármacos: una herramienta prometedora contra la tuberculosis

“…Actualmente, las técnicas de producción de nanofibras son variadas, siendo el electrohilado la más utilizada (52) . El uso de nanofibras para el tratamiento de la TB u otras micobacteriosis es un campo fértil de investigación, se han incorporado fármacos como estreptomicina, isoniacida, pirazinamida y claritromicina con resultados variables (53) . Sin embargo, unas películas diseñadas para la administración oral de isoniacida demostraron una alta eficiencia de desintegración, liberación y encapsulamiento del fármaco (54) .…”

Antifungal nanofibers made by controlled release of sea animal derived peptide

“…Despite the Cm-p1 activity, previous results 11 presented higher activity than 10% Cm-p1-PVA nanofibers. According to Hassounah and co-workers, 41 the establishment of hydrogen bonds between the amino groups of the drugs and the alcohol groups of PVA can lead to deactivation of the drugs due to the high polarity of the alcoholic oxygen atom in PVA. 41 In a preceding theoretical structural analysis, 11 it was predicted that Cm-p1 consists of a hydrophilic molecule scoring an impressive average of hydropathicity and displays a minor central hydrophobic region bordered by basic amino acids at the extremes.…”

“…According to Hassounah and co-workers, 41 the establishment of hydrogen bonds between the amino groups of the drugs and the alcohol groups of PVA can lead to deactivation of the drugs due to the high polarity of the alcoholic oxygen atom in PVA. 41 In a preceding theoretical structural analysis, 11 it was predicted that Cm-p1 consists of a hydrophilic molecule scoring an impressive average of hydropathicity and displays a minor central hydrophobic region bordered by basic amino acids at the extremes. 11 A three-dimensional theoretical model of Cm-p1 revealed an α-helix conformation with a distribution of net charge caused by exposed cationic histidine (His8) and arginine (Arg2 and Arg10) residues.…”