Colloidal carriers for extended absorption window of furosemide.

OBJECTIVES

The aim was to investigate the potential of self-microemulsifying drug delivery systems (SMEDDS) and niosomes as carriers for widening the gastrointestinal absorption window of furosemide (model acidic drug).

METHODS

The drug was incorporated in SMEDDS and was encapsulated into niosomes. The intestinal absorption was monitored at two anatomical sites (duodenum and jejuno-ileum). This employed in situ rabbit intestinal perfusion technique.

KEY FINDINGS: Perfusion of drug solution (control) revealed poor intestinal permeability with per cent fraction absorbed (%Fa) from the duodenum and jejuno-ileum being 1.3 and 0.6 % per cm, respectively. Formulation of furosemide as SMEDDS increased the %Fa from the duodenum and jejuno-ileum to reach 1.7 and 1 % per cm, respectively. Niosomal encapsulation increased the %Fa from duodenum and jejuno-ileum to record 1.9 and 1.2 % per cm, respectively. The increase in the %Fa was also revealed as a reduction in the length required for 95 % absorption of the drug which was reduced from 557.2 to 245.8 cm and to 279.8 cm after delivery as niosomes or SMEDDS, respectively, in case of jejuno-ileum. The same trend was recorded with the duodenum.

CONCLUSION

The recorded results highlighted the potential for SMEDDS and niosomes for widening the absorption window of acidic drugs after oral administration.