The combination of hydroxypropylmethylcellulose acetate succinate and L-lysine into ternary amorphous solid dispersions of quercetin to enhance its dissolution

Abstract

The purpose of this study was to enhance quercetin (Que) dissolution by preparing its ternary amorphous solid dispersions. The ternary amorphous solid dispersions were prepared by solvent evaporation method using hydroxypropylmethylcellulose acetate succinate (HPMCAS) and L-lysine (lys) as the carriers. The effect of the combination of polymer and amino acid on nucleation inhibition was evaluated by the nucleation induction time. Supersaturation tests were used to investigate the ability of maintaining Que supersaturation of the combination of polymer and lys. The dissolution results showed that the dissolution effect of ternary solid dispersions was better than binary solid dispersions. Stronger crystallization inhibition didn't lead to better dissolution effect and the dissolution of the prepared amorphous solid dispersions of Que was carrier-controlled. Lys modified the dissolution microenvironment of the solid dispersions, which made drug dissolution in the optimal pH environment, and effectively improved drug dissolution. Polymer/lys can be one of the most potential carriers for preparing amorphous solid dispersions of Que.

Keywords

• Quercetin
• Hydroxypropylmethylcellulose acetate succinate
• Lysine
• Supersaturation
• Amorphous solid dispersion
• Dissolution