A gellan gum derivative as in-situ gelling cationic polymer for nasal drug delivery.

The aim of the present study was the development of a novel gellan gum derivative exhibiting mucoadhesive properties for nasal application. Accomplishing this, amino groups have been introduced to the polymeric backbone. The resulting synthesis products were characterized in terms of the amount of attached amino groups, regarding hydration, zeta potential and gel characteristics. Mucoadhesiveness was assessed studying rheological synergism, by rotating cylinder and regarding tensile studies. Next to erythrocyte-/cytotoxicity evaluation, the impact on ciliary beat frequency of nasal epithelial cells was investigated. Results revealed coupling rates up to 1259.50 ± 75.98 μmol/g polymer as well as accelerated hydration of the derivatives. Comparing aminated with unmodified gellan, enhanced mucoadhesion was verified by a 32-fold increase in viscosity of polymer/mucus mixtures and by a 14-fold extended mucosal adhesion time. Tensile studies demonstrated a 9-fold higher total work of adhesion and a 3.75-fold elevated maximum detachment force. Cellular membrane was not seriously impaired. CBF studies proved a reversible inhibition due to the application of the novel derivative. According to the outlined findings, aminated gellan gum can be considered as a promising excipient for nasal dosage forms improving drug bioavailability by superior adhesive features.

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