Preparation & Characterization of Sustained-release Floating Microsphere of Digestive Enzymes

Abstract

Introduction: Pepsin is a proteolytic enzyme which is widely used as a digestive aid. Its dose is 300 mg - 1 gm per day in divided doses. Its biological half-life is around 3.5 hrs. Pepsin is active only in the acidic pH of the stomach; its activity decreases tremendously in the basic pH. So, it is required to retain in the stomach for maximum proteolytic activity. The goal of the current effort is to develop and assess an oral controlled floating drug delivery system for pepsin that will shorten its stay in the stomach and result in a longer effect. Methods: The 12-hour sustained effect of pepsin floating microspheres was planned. This also improves the stability of the Pepsin by immobilizing them on the microsphere. Pepsin is widely used in chronic gastritis, so developing a floating drug delivery system is therefore necessary. In light of the aforementioned principles, a critical need for the creation of a dosage form to administer Pepsin in the stomach and boost the enzyme's effectiveness, enabling sustained action, was identified. The current study used a methodical strategy to create floating microspheres of Pepsin dosage forms. Results: Optimization was done for floating ability, yield, entrapment efficiency, and release study using different concentrations of ethylcellulose & HPMC E4M. For parameter optimization and to demonstrate the significant impact of variables, 32 full factorial designs were used. The manufactured microspheres had good encapsulation rates, excellent floating, & excellent micromeritic properties as single-unit dosage forms. Conclusion: It has been demonstrated that pepsin prepared as floating microspheres can be used to improve proteolytic activity and extend pepsin's gastric residence.