In-vitro Evaluation and Optimization of Sacubitril and Valsartan Floating Tablet using Natural Polymer

Abstract

Oral systems have become gradually extensive for human consumption because of their numerous advantages, such as formulation efficiency, cost-effectiveness, and patient safety compliance. These systems offer a versatile platform for controlled drug release, allowing precise targeting of absorption site in the gastrointestinal tract. Accomplishing ideal therapeutic results for certain medications often requires precise control of drug release at specific locations within the gastrointestinal tract. In this study, our goal was to create a floating drug delivery system for two vital cardiovascular medications, sacubitril and valsartan. Our specific objectives were to extend floating time, prolong stomach residency, and reduce floating lag time. The strategy involved harnessing the synergistic potential of natural polymers in optimal proportions to enhance drug activity. Following the principles of quality by design (QbD), we systematically explored various formulation factors to optimize the drug delivery system. Analysis of tablet characteristics revealed significant variations in key parameters, such as swelling index, floating lag time (FLT), total floating time (TFT), and drug content for both sacubitril and valsartan. The enhanced formulation (F12) stood out with a remarkable swelling index of 93.4%, a floating lag time of 6.7 seconds, and an impressive total floating time of 12 hours. Furthermore, high drug content percentages were achieved, with sacubitril at 98.70% and valsartan at 94.65%. The successful development and optimization of the floating tablet formulation carry substantial clinical implications. The extended gastric retention, controlled drug release, and high drug content of the optimized formulation suggest enhanced bioavailability and therapeutic efficacy for both sacubitril and valsartan. The prolonged total floating time offers convenience to patients, potentially improving medication adherence in managing cardiovascular diseases. In conclusion, this study highlights the formulation and optimization of floating tablets as a noteworthy advancement in drug delivery technology, promising improved therapeutic outcomes and enhanced patient convenience.