Enhancement of anti-inflammatory activity of glycyrrhizic acid by encapsulation in chitosan-katira gum nanoparticles

• Glycyrrhizic acid loaded chitosan-katira gum nanoparticles made by ionic complexation.
• Response surface methodology 3-factor, 3-level central composite design used.
• Size of optimized nanoparticles as observed in TEM was below 80 nm.
• Hurdles hindering anti-inflammatory activitiy of glycyrrhizic acid overcome.

Efforts were made to improve the bioavailability and efficacy of Glycyrrhizic acid, a triterpentine saponin obtained from Glycyrrhiza glabra, having several pharmacological properties, by its encapsulation in biocompatible biopolymeric nanoparticles. Polycationic chitosan and polyanionic gum katira were used to prepare nanoparticles by ionic complexation method. Glycyrrhizic acid was loaded into the nanoparticles and was then examined for change in its in vivo anti-inflammatory activity against carrageenan-induced rat hind paw inflammation. The effects of concentrations of glycyrrhizic acid, chitosan and katira gum, upon particle size and encapsulation efficiency of glycyrrhizic acid were studied with the help of response surface methodology employing 3-factor, 3-level central composite experimental design. Particle size and encapsulation efficiency of optimized nanoparticulate formulation were 175.8 nm and 84.77%, respectively. Particles were observed in transmission electron microscopy to be spherical in shape and 80 nm in size. FTIR analysis indicated electrostatic interactions between carboxyl groups of ammonium glycyrrhizinate and amino groups of chitosan. In vitro drug release studies indicated that glycyrrhizic acid was released from the nanoparticles following zero-order kinetics and that there was a sustained release of the drug with 90.71% of it being released over a 12 h period, and that the mechanism of release of glycyrrhizic acid from the nanoparticles was a combination of diffusion and erosion of the polymer matrix. In-vivo anti inflammatory efficacy of glycyrrhizic acid clearly improved upon encapsulation in chitosan-katira gum nanoparticles, by overcoming the limited bioavailability of its other forms.

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