Formulation and Evaluation of Nisoldipne Sublingual Tablets Using Pullulan & Chitosan for Rapid Oromucosal Absorption

Nisoldipine (NSD) is a calcium channel blocker used for treatment of angina pectoris, hypertension and congestive heart failure etc. It belongs to BCS class-II i.e., low solubility & low bioavailability (3.7 to 8.4%) due to extensive pre-systemic metabolism of NSD. Therefore, this research work was carried out with aim to improve solubility and bioavailability. NSD sublingual tablets were prepared by direct compression method with two biodegradable polymer as major components, pullulan as solubility enhancer & chitosan used to reduce flushing action of saliva and further evaluated pre & post-compression parameters, in-vitro drug release study and characterised by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) & Fourier transform infrared spectroscopy (FTIR). It was observed that, formulation F3 containing 3 % w/w of pullulan and 4% w/w chitosan showed satisfactory results with disintegration time of 34 second, wetting time of 20 second and dissolution (98.45%) in 45 min. The DSC, XRD & FTIR studies showed no interaction between drug and polymer or with other additives. For rapid absorption and high bioavailability, with subsequent almost immediate onset of pharmacological effect. From this study, It can be concluded that, drug having low solubility and low bioavailability due to pre-systemic metabolism can be improve by cost effective, easy to scale up sublingual oro-mucosal approach.