Gellan-thioglycolic acid conjugate: Synthesis, characterization and evaluation as mucoadhesive polymer

Gellan-thioglycollic acid conjugate was synthesized with the objective to improve its mucoadhesive properties. Synthesis of conjugate was confirmed by -SH stretch in the Fourier-transform infrared spectra at 2571 cm(-1). It was found to contain 13.92 mM of thiol groups/g of the conjugate. Thiolation of gellan gum was found to slightly increase its degree of crystallinity and decrease its sensitivity to Ca2+-induced gelation. On screening of gellan-thioglycollic acid conjugate for ex-vivo ocular tolerance using hen's egg chorio-allantoic membrane test and for biocompatibility by resazurin assay on Vero-cells, it was found to be non-irritant and biocompatible. Metronidazole gels formulated using gellan thioglycollic acid conjugate as bioadhesive agent showed 1.82-fold higher mucoadhesive strength than the gels formulated using gellan gum. Further, the metronidazole gels containing gellan and gellan-thioglycollic conjugate released the drug following first-order and Higuchi's square-root release kinetics. In conclusion, gellan-thioglycollic acid conjugate is a promising bioadhesive excipient. (C) 2013 Elsevier Ltd. All rights reserved.