Abstract

5-FLUOROURACIL MUCOADHESIVE LIQUID SUPPOSITORY FORMULATION AND EVALUATION

*Hanan J. Kassab, Yehia I. Khalil

Abstract

5-FU was formulated into a thermo-sensitive liquid suppository in combination with citrus pectin as Galectin-3 inhibitor, using poloxamer P407 as a thermo- gelling agent. Pectin addition retarded 5-FU solubility but the addition of cyclodextrin improved it, due to complex formation and decrease in crystallinity of 5-FU from 100 to 19.01% confirmed by XRD and FTIR. All the formulas showed sustained release due to P407 incorporation and non-Fickian release kinetics. The incorporation of carbopol C940 as a mucoadhesive polymer altered the gelation temperature of P407. The selected liquid suppository formula P4( P407:C940(19:1)) exhibited mucoadhesion strength of 2.476×103 dyne/cm2 ,gelation temperature of 31.7°C and gel strength of 75 sec and showed pseudo-plastic flow with consistency of 3.7255 and 3.9934 mPa.s-n at 20° and 37° C respectively and permeation through sheep rectal tissue of 0.695cm/hr.

Keywords: 5-FU, Pectin, Poloxamer 409, Carbopol 940, Rectal Cancer.