Synthesis, characterization, and in vitro evaluation of gamma radiationinduced PEGylated isoniazid

Background: The search for innovative anti-tubercular agents has received increasing attention in tuberculosis chemotherapy because Mycobacterium tuberculosis infection has steadily increased over the years. This underlines the necessity for new methods of preparation for polymer-drug adducts to treat this important infectious disease. The use of poly(ethylene glycol)(PEG) is an alternative producing anti-tubercular derivatives. However, it is not yet known whether PEGylated isonicotinylhydrazide conjugates obtained by direct links with PEG are useful for therapeutic applications. Results: Here, we synthesized a PEGylated isoniazid (PEG-g-INH or PEG­INH) by gamma radiation-induced polymerization, for the first time. The new prodrugs were characterized using Raman and UV/Vis spectrometry. The mechanism of PEGylated INH synthesis was proposed. The in vitro evaluation of a PEGylated isonicotinylhydrazide macromolecular prodrug was also carried out. The results indicated that PEG­INH inhibited the bacterial growth above 95% as compared with INH, which showed a lower value (80%) at a concentration of 0.25 µM. Similar trends are observed for 0.1, 1, and 5 µM. Conclusions: In summary, the research suggests that it is possible to covalently attach the PEG onto INH by the proposed method and to obtain a slow-acting isoniazid derivative with little toxicity in vitro and higher antimycobacterial potency than the neat drug.

Poly(3-hydroxybutyrate) graft copolymer dense membranes for human mesenchymal stem cell growth

Background: The use of novel materials as an artificial extracellular matrix for stem cell growth is a current strategy of increasing interest for regenerative medicine. Here, we prepare thermal-remolded membrane scaffolds from poly(3-hydroxybutyrate) grafted with 2-amino-ethyl methacrylate hydrochloride. However, it is unclear whether these membranes are useful for tissue engineering. Results: The mechanical properties, tribology, and morphology of the dense membranes were assessed. The results show that tensile strain at break and roughness of the compressed membrane decrease with increasing graft degree. Moreover, graft copolymer membranes showed lower resistance to scratching, greater degree of swelling and higher brittleness than un-grafted P(3HB) films. Thus, it effectively supports the growth of dermal fibroblast, as demonstrated by epifluorescence microscopy. Conclusions: It is concluded that the developed membrane can be properly used in is the restoration of skin tissue. How to cite: González-Torres M, Sánchez-Sánchez R, Solís-Rosales SG, et al. Poly(3-hydroxybutyrate) graft copolymer dense membranes for human mesenchymal stem cell growth.