Development and in vitro characterization of niosomal formulations of immunosuppressant model drug

ABSTRACT

Among immunosuppressive agents cyclosporine A is drug of unique importance. This drug has a low therapeutic index, and it has many toxic effects. After oral administration its absolute bioavailability is variable due to poor absorption. Niosomes are new and versatile carriers to deliver drug. The bioavailability of immunosuppressant drug cyclosporine A can be increased by niosomal drug delivery system. So our basic theme was to prepare niosomes of immunosuppressant drug using cholesterol, span 60 and tween 60 etc. Niosomes were characterized for zeta potential, size, poly dispersivity index [PDI], entrapment efficiency and In vitro release profiles. Six niosomal formulations [F1-F6] were successfully developed using thin film hydration technique. Among various formulations F2 showed the highest entrapment efficiency 77.29 %. The DSC thermograms of physical mixtures and niosomal formulations indicated the presence of drug in crystalline form. In vitro drug release study demonstrated higher drug release values as compared to drug aqueous dispersion. Niosomal formulations were capable of releasing drug in sustained manner. The overall results demonstrated that developed niosomal carriers are competitive candidates for improving dissolution profile of cyclosporine A leading to increased bioavailability at the site of action