Development, Optimization and Evaluation of Bisoprolol Fumarate Loaded Self Emulsifying Drug Delivery System

Abstract

In the current research, a Bisoprolol Fumarate-loaded Self-Emulsifying Drug Delivery System (SEDDS) was developed to enhance the solubility and bioavailability of the drug, aiming to overcome its pharmacokinetic limitations. Various oils, surfactants, and co-surfactants were evaluated for their solubilizing capacity, and a pseudo-ternary phase diagram was constructed to identify the optimal emulsification region. Eight formulations (F1 to F8) were prepared and subjected to thermodynamic stability, emulsification time, droplet size, zeta potential, and polydispersity index (PDI) analysis. The optimized formulation (F8) demonstrated thermodynamic stability, rapid emulsification, droplet size of 204.7 ± 5.0 nm, and zeta potential of −13.38 ± 1.5 mV.

In-vitro drug release studies showed that the SEDDS formulations exhibited a significantly faster and more complete release of Bisoprolol Fumarate compared to the pure drug, achieving over 85% release within 15 minutes in pH 1.2 buffer and 90% release in pH 6.8 buffer within 60 minutes. The pharmacodynamic study using a hypertensive rat model revealed that the SEDDS formulation (F8) achieved equivalent antihypertensive efficacy to the marketed formulation, even at half the dose, due to improved drug absorption and bioavailability.

The study concludes that the Bisoprolol Fumarate-loaded SEDDS provides a promising strategy for enhancing the drug's bioavailability and therapeutic efficacy, especially in managing hypertension and cardiovascular conditions.