European Journal of Biomedical and Pharmaceutical Sciences

MUCOADHESIVE BUCCAL TABLETS OF NISOLDIPINE FOR ORAL DELIVERY: PREPARATION, IN-VITRO AND IN-VIVO EVALUATION

Sk. Wajid and Ajmeera Ramarao*

ABSTRACT

Nisoldipine (ND) is calcium channel blocker used in treatment of hypertension. ND has poor oral bioavailability (BA) of about 5% due to extensive first-pass metabolism and limits its therapeutic use. Hence, the buccal delivery was considered as an alternative used to enhance the BA of ND. ND buccal tablets (ND-BT) were prepared by direct compression technique, using carbopol 934P HPMC K4M and K15M as muco-adhesive polymers. Prepared ND-BT formulations were evaluated for an optimized system based on physico-chemical, ex-vivo residence time, in-vitro and ex vivo permeation studies. Further, in vivo studies of optimized ND-BT were conducted in pig’s comparison with ND marketed formulation. The evaluation parameters of the tablets were within the pharmacoepial acceptable limits. However, the swelling and bio-adhesive strength were increased with increasing polymer concentrations. From the in-vitro release studies it is shown that, tablets with HPMC K4M (N2) exhibited better release profile than all other formulation, and were considered as optimized BT formulation. The release mechanism from kinetic methods suggests that, the drug release follows zero-order kinetics with diffusion mechanism. Further, about 2.63-folds enhancement in the oral bioavailability of ND from buccal tablet was observed when compared with marketed formulation. Thus, the buccal tablets of ND showed enhanced BA and could be another delivery approach for oral administration.

Keywords: Nisoldipine, first-pass metabolism, Buccal tablets, in vitro, ex vivo, in vivo.