Design and evaluation of solid self-emulsifying drug delivery system of rosuvastatin calcium

Abstract

Background: The work has been undertaken with an objective to prepare a self-emulsifying drug delivery system (SEDDS) of rosuvastatin calcium (ROS) with the least amount of surfactant which could enhance its solubility and oral bioavailability.Materials and Methods: Spectrophotometric method was used to estimate the solubility of the drug in various oils, surfactant and co-surfactant. The phase behavior and most efficient self-emulsifying region were identified by constructing pseudo ternary phase diagram. The solid-SEDDS (S-SEDDS) was prepared using an adsorbent consequently the prepared S-SEDDS were filled up in hard gelatin capsule which were evaluated for various physicochemical parameters.Results: The composition of optimized formulation consisted of 10 mg of ROS, capmul MCM (oil), cremophor ELP (surfactant) and propylene glycol (co-surfactant). The optimized formulation showed negative zeta potential (−22.11 mv), optimal particle size (10.59 nm) and demonstrated excellent self-emulsifying ability with a maximum solubilizing capability. The S-SEDDS formulations were prepared from the optimized liquid SEDDS, which revealed maximum release rate (97.7%) among all the prepared S-SEDDS formulation and marketed formulation.Conclusion: It was concluded that S-SEDDS prepared from liquid SEDDS can be a promising novel approach to enhance the solubility and drug release of ROS, which in turn also develops a stable formulation, least drugs leakage and precipitation than the liquid SEDDS.

Keywords: Adsorbent; bioavailability; drug release; rosuvastatin calcium; self-emulsifying drug delivery system; solubility