Development of amino acid salt-based curcumin@lysine acetate co-amorphous system using liquid-assisted grinding for improved solubility and dissolution

Authors

Udaykumar Patil
Snehal Rawal
Jidnyasa Pantwalawalkar
Sopan Nangare
Dilip Dagade
Pravin Patil
Namdeo R. Jadhav

Abstract

Curcumin, multivalued phytoceutical, exhibits appreciable safety. However, its therapeutic utility is significantly compromised due to low aqueous solubility, and thus, poor absorption and low bioavailability become apparent. To surpass this limitation, the present work aims to develop amino acid salt-based curcumin@lysine acetate co-amorphous system for improved solubility and dissolution. Initially, screening of curcumin-amino acid mixtures was performed for saturation solubility assessment. Considering the outcome, lysine acetate was formulated to generate a co-amorphous mixture (COAM) by liquid-assisted grinding and evaluated for saturation solubility and different spectroscopical characterizations. Curcumin-lysine acetate COAM tablet formulation was developed by direct compression method and evaluated for appearance, thickness, hardness, weight variation, friability, drug content, disintegration, and in vitro dissolution studies. Further, curcumin-lysine acetate COAM and tablet formulation were screened for the accelerated stability study. Resultantly, curcumin-lysine acetate binary mixture demonstrated the highest saturation solubility among screened curcumin-amino acid binary mixtures that might be ascribed to the hydrotropic properties of lysine acetate. Moreover, 476-fold solubility enhancement in water was observed by curcumin-lysine acetate COAM. Later, the amorphization of the curcumin-lysine acetate COAM was confirmed using Fourier-transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction. COAM tablet formulation showed optimum evaluation characteristics with improved drug dissolution. Therefore, the amino acid salt-based co-amorphous system can be used for solubility and dissolution improvement of curcumin and other multivalued phytoceutical.

Publisher

Faculty of Pharmaceutical Sciences, Chulalongkorn University

First Page

711

Last Page

719

Recommended Citation

Patil, Udaykumar; Rawal, Snehal; Pantwalawalkar, Jidnyasa; Nangare, Sopan; Dagade, Dilip; Patil, Pravin; and Jadhav, Namdeo R. (2023) "Development of amino acid salt-based curcumin@lysine acetate co-amorphous system using liquid-assisted grinding for improved solubility and dissolution," The Thai Journal of Pharmaceutical Sciences: Vol. 46: Iss. 6, Article 11.
Available at: https://digital.car.chula.ac.th/tjps/vol46/iss6/11