In situ gastric floating gel of atazanavir sulphate for sustained release: formulation, optimization and evaluation

Abstract

Aim: Atazanavir sulphate belongs to BCS class II drug, its oral bioavailability is limited due to its rapid first-pass metabolism and P-gp efflux. Materials & methods: The in situ floating gel using the complexed drug was prepared by ion gelation method and optimized the formulation as per 32 full factorial design. Results: Floating lag time of optimized formulation was found to be 18 s and percentage drug release of 94.18 ± 0.18 % at the end of 16 h. The concentration of gelling polymer affects drug release and a floating lag time and vice versa. Conclusion: In situ floating gel of atazanavir sulphate was found promising to sustain drug release due to an increased gastric residence time, which leads to enhanced potential therapy.