Gellan co-polysaccharide micellar solution of budesonide for allergic anti-rhinitis: An in vitro appraisal

• Novel amphiphilic gellan co-polysaccharide was synthesized and characterized.
• Co-polysaccharide formed stable, spherical nanomicellar structures in water.
• Nanomicelles incorporated >95% budesonide in their lipophilic core.
• Maximum 50% drug released into simulated nasal fluid (pH 5.5) in 6 h.
• Micellar solution of budesonide could avoid adverse events of anti-rhinitis.

The aim of this study was to design a novel amphiphilic co-polysaccharide for the development of anti-rhinitis micellar solution of budesonide. Herein, a long alkyl chain (C18) was successfully grafted onto gellan polysaccharide by etherification reaction. The dispersion of co-polysaccharide in water led to formation of spherical, nanomicellar structures. Depending upon the co-polysaccharide:drug weight ratio (1:1, 1:2 and 1:3), a maximum drug loading (>95%) was noted at the lowest level. The nanomicelles were in the range of 371–750 nm and showed negative zeta potential (−48.3 to −67.2 mV) values indicating their stability in aqueous system. They exhibited a longer dissolution profile in simulated nasal fluid (pH 5.5). The dissolution efficiency (39.79 ± 0.93%) was maximal at the lowest polymer: drug ratio in 6 h. The drug release was found to follow first order kinetic model. Korsmeyer-peppas modeling of in vitro drug release data indicated that besides simple diffusion, no other physical phenomenon was involved in the event of drug release from the nanostructures. Differential scanning calorimetry analysis suggested some degree of physical incompatibility; however Infrared spectroscopy revealed chemical compatibility between drug and co-polysaccharide. Thus, the co-polysaccharide micellar system offers a splendid outlook in controlled intranasal delivery of budesonide for the symptomatic relief of anti-rhinitis.