Design and optimization of pellets formulation containing curcumin ascorbic acid co-amorphous mixture for ulcerative colitis management

Abstract

Curcumin is known for its various therapeutic properties like anti-inflammatory, antioxidant, anticancer, however, its oral use is restricted due to its low solubility and dissolution rate in alkaline pH. In this study co-amorphous mixture of curcumin–ascorbic acid (CU:AA) of different molar ratios was prepared using the ball milling method. The solubility and characterization of the mixture were studied using FTIR, DSC, and XRD study. Mixture (1:0.50) molar ratio showed the highest solubility and was formulated in pellets dosage and optimized using 3² full factorial designs. The solubility results revealed that a significant increase (p < 0.005) in the solubility of curcumin by the ratio 1:0.50 (212 ± 12 µg/ml) compared to the pure drug (90.0 ± 10 µg/ml). XRD and DSC studies confirmed the formation of amorphous curcumin, whereas FTIR elucidated weak hydrogen interactions. In-vitro dissolution study results showed the (CU:AA) ratio (1:0.50) higher percent drug release (81.61 ± 5.12%) compared to the pure drug (19.44 ± 4.60%). The developed formulations are found to be stable. Therefore, the prepared pellets of co-amorphous mixture enhance the solubility, dissolution rate, and stability of curcumin in higher pH, which will become a promising approach for combination therapy in the treatment of ulcerative colitis patients.

Acknowledgment

The authors are grateful to the Government College of Pharmacy, Aurangabad, India for providing the facilities to conduct the research.

Disclosure statement

The authors declare no potential conflict of interest.