Nashiru Billa
University of Nottingham, Malaysia
Title: Food Effects on gastrointestinal transit properties of Amphotericin B solid lipid nanoparticles
Biography
Biography: Nashiru Billa
Abstract
Amphotericin B (AmB) is a polyene antifungal agent highly effective in treating life-threatening systemic fungal infections. We aimed to formulate AmB solid lipid nanoparticles (SLNs) meant for oral delivery and to study the effect of food on the absorption of AmB at the various regions of the gastrointestinal tract using an indirect approach. The indirect estimation utilises paracetamol (PAR) and sulphapyridine (SP) as marker drugs; the SP being a metabolic product of sulphasalazine (SSZ) from the activity of colonic flora. AmB, PAR and SSZ were similarly formulated into SLNs which showed identical physical properties (size, surface charge and morphology) and were simultaneously administered to fasted and fed rats whilst blood samples were withdrawn from their tails simultaneously for HPLC analysis. Cmax was increased by almost twofold and AUC0-30 by more than twofold from AmB SLN compared with AmB suspension however Tmax was increased (0.25 hr vs 4 hr). The presence of food delayed Tmax and significantly (p<0.05) decreased Cmax for the absorption of AmB from the AmB SLN although oral bioavailability (7953 ng.hr/mL vs 7565.33 ng.hr/mL) was not significantly reduced. The plasma concentration-time curves of PAR and SP were used in marking the approximate times at which AmB absorption occurred in the small intestines and colon respectively. The small intestines and the colon showed significant absorption of AmB SLN however, absorption in the colon was considered as partly due to slow drug release into blood from lymphatic drainage in the small intestines. The differences in the estimated percentage absorption of AmB SLNs in the stomach, small and large intestines for both the fasted and fed rats were not statistically significant. We may conclude that improved oral absorption of AmB was achieved following incorporation in SLN and food did not significantly affect the absorption of the AmB SLN from the gastrointestinal tract