Abstract
Studies related to loading ability and delivery of clinically used first-line anti-tuberculosis drugs (ATDs) such as isoniazid, rifampicin, pyrazinamide and streptomycin on the surface of starch-derived bulk and nanopolyurethanes (SBPUs and SNPUs) as drug delivery systems (DDS) have been focused to minimise or remove the drug-associated adverse effects. The efficiencies of nanopolyurethanes obtained from the differently substituted cyclic aliphatic and aromatic isocyanates have been studied for drug loading and release purposes. Different advanced instrumental techniques analysed the structural and morphological properties, thermal stability and crystallinity of the starch nanopolyurethans. Average particle sizes ranging from 27.35–42.38 nm to 126.89–218.60 nm for starch nanopolyurethans, SNPU3i and SNPU4i, respectively, were determined by high-resolution transmission electron microscopy. Similarly, the loading efficiency of ATDs to the surfaces of SNPUs and SBPUs was observed in the range of 60–97% while ATDs-loaded SNPUs showed a sustainable release profile for all ATDs except for streptomycin. However, most SBPUs provided burst-release for all the above-mentioned ATDs in pH-dependent studies. The anti-tuberculosis assay against the Mycobacterium tuberculosis H37Rv strain revealed that streptomycin-loaded SNPU4i and isoniazid-loaded SNPU7i are approximately 42 and 7 times more active than the native streptomycin and isoniazid, respectively.
Highlights
Studies related to loading ability and delivery of clinically used first-line anti-tuberculosis drugs (ATDs) such as isoniazid, rifampicin, pyrazinamide and streptomycin on the surface of starch-derived bulk and nanopolyurethanes (SBPUs and starchderived nano polyurethanes (SNPUs)) as drug delivery systems (DDS) have been focused to minimise or remove the drug-associated adverse effects
Chemical structures of the starch-derived bulk polyurethanes (SBPUs) were corroborated by 1H NMR and FT-IR. 1H NMR signals corresponding to –NH group of the urethane linkages [–NH–(CO)–O–] and starch backbone of SBPU5i-7i were observed in the range of δ 7.1–8.5 and δ 3.0–5.8 ppm, respectively
For the case of SBPU6i-7i obtained from cyclic aliphatic isocyanates, the methylene protons of the cyclic backbone were observed in the range of ~ δ 2.63–0.73 ppm
Summary
Studies related to loading ability and delivery of clinically used first-line anti-tuberculosis drugs (ATDs) such as isoniazid, rifampicin, pyrazinamide and streptomycin on the surface of starch-derived bulk and nanopolyurethanes (SBPUs and SNPUs) as drug delivery systems (DDS) have been focused to minimise or remove the drug-associated adverse effects. The inclusion of new drug delivery devices or improving the bioavailability, stability, target-oriented modification, drug distribution, metabolism, availability of drugs at the infected site, therapy time, drug resistance, and so on for the existing TB drugs would be more economical and beneficial In this direction, polyurethanes-based versatile materials, which are one of the most ubiquitously applied polymers in different fields, may be explored as a drug delivery system (DDS)[7] for anti-tuberculosis drug delivery. The urethane-functionalized starch in bulk and nano state acted as potential drug delivery devices in the field of sustained-release of drug molecules[20,21,22,23] That, these covalently cross-linked polyurethanebased starch nanoparticles are capable to show the high load-carrying capacity of the drug in the physiological medium with improved stability and b iodegradability[24,25,26,27,28]. It is relevant to mention that starch nanopolyurethans are found as a better adsorbent for biodiesel purification than that of simple SNCs as per or earlier s tudies[29,30]
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