Synthesis, antibacterial activity, and sustainable release of novel α-aminophosphonate derivatives loaded carrageenan cryogel.

Synthesis, antibacterial activity, and sustainable release of novel α-aminophosphonate derivatives loaded carrageenan cryogel.

Int J Biol Macromol. 2020 Jun 29;:

Authors: Elsherbiny DA, Abdelgawad AM, El-Naggar ME, El-Sherbiny RA, El-Rafie MH, El-Sayed IE

Abstract
Novel α-aminophosphonates 4 were synthesized via one pot three-component reaction of 4-aminoantipyrine, aldehydes, triphenylphosphite and Lewis acid catalyst. The chemical structures of all the synthesized compounds were elucidated by IR, NMR and MS spectral analysis. The antimicrobial activity of 4 was tested in vitro against pathogenic microbes such as Escherichia coli, Staphylococcus aureus, Aspergillus niger and Candida albicans. Three of them (4f-h) exhibited high antimicrobial activity and were loaded to Carrageenan cryogel for drug delivery studies. With the aid of cellulose nanofibrils (CNF) as reinforcing material and glyoxal as a cross-linking agent, porous cryogels with improved mechanical properties were obtained. Among all, CAR-7 presents the optimum cryogel sample, which contained around 16% CNF and 0.2 mL/15 mL polymer blend. CAR-7 demonstrated highest mechanical compressive strength, porosity (80%), and 75% swelling capacity. Sustainable release behavior over 24 h was observed for the loaded cryogels. The antibacterial activity of cryogels against Staphylococcus aureus showed marginal differences between samples. CAR-9 (loaded with 4f) showed the highest reduction percentage in number of bacterial colonies (99.94%) followed by CAR-11 (loaded with 4h, 99.3%) and finally CAR-10 (loaded with 4g, 99.29%) when compared to the control.

PMID: 32615220 [PubMed – as supplied by publisher]

Source: Industry