Lignin and Cellulose Blends as Pharmaceutical Excipient for Tablet Manufacturing via Direct Compression

Extensive efforts are being made to find alternative uses for lignin (LIG). In the present work the use of this biopolymer as an excipient to prepare tablets was studied.

For this purpose, LIG was combined with microcrystalline cellulose (MCC) and used as excipients to prepare directly compressed tablets containing a model drug, tetracycline (TC). The excipients contained different
concentrations of LIG: 100%, 75%, 50%, 25% and 0% (w/w). Two different compression forces were
used (two and five tonnes).

When formulations were prepared using LIG as the only excipient,tablets were formed, but they showed lower densities and crushing strength than the ones obtained with only MCC or LIG/MCC blends. Moreover, tablets prepared using five tonnes of compression force showed TC releases ranging from 40% to 70% of the drug loading. On the other hand, the tablets prepared using two tonnes of compression force showed a faster and more efficient TC release,
between 60% and 90%.

The presence of LIG in the tablets modified significantly the release profile and the maximum amount of TC released. Finally, a DPPH (2,2-diphenyl-1-picrylhydrozyl) assay was performed to confirm that the presence of LIG provided antioxidant properties to the formulations. Accordingly, LIG has potential as a pharmaceutical excipient.

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Domínguez-Robles, J.; Stewart, S.A.; Rendl, A.; González, Z.; Donnelly, R.F.; Larrañeta, E. Lignin and Cellulose Blends as Pharmaceutical Excipient for Tablet Manufacturing via Direct Compression. Biomolecules 2019, 9, 423.