Advances in Pharmacology and Pharmacy 1(1): 18-25, 2013 http://www.hrpub.org DOI: 10.13189/app.2013.010104 Formulation and Evaluation of Nisoldipne Sublingual Tablets Using Pullulan & Chitosan for Rapid Oromucosal Absorption Vivekanand K. Chatap * , Abhishek R. Maurya, Prashant K. Deshmukh, Laxmikant R Zawar Department of Pharmaceutics & Industrial Pharmacy, H.R Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra, India- 425405 Corresponding Author: chatap@rediffmail.com Copyright © 2013 Horizon Research Publishing All rights reserved. Abstract 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. Keywords Nisoldipine, Sublingual Tablet, Pullulan, Chitosan and Oromucosal Absorption 1. Introduction Nisoldipine [(±)-3-isobutyl-5-methyl-1,4-dihydro-2,6-dimethyl-4-(2-nitr ophenyl) pyridine-3,5-dicarbox-ylate (Fig 1)] is a calcium antagonist of the 1,4- dihydropyridine family with non-symmetrical ester functions belong to antihypertensive category drug, which reduces vascular resistance, blood pressure by inhibiting calcium uptake by the myocardium and smooth muscle cells. NSD has poor solubility, high permeability and high hepatic metabolism (1) belonging to Class II of biopharmaceutical classification system (BCS) and biopharmaceutical drug disposition system (BDDCS) and used for the treatment of angina pectoris, hypertension and congestive heart failure (2). It has a low systemic bioavailability (3.7 to 8.4%) due to extensive pre-systemic metabolism. Sublingual administration can offer an attractive and promising alternative route of administration of drug with low bioavailability (3). An advantage of the sublingual drug delivery system, drug can be directly absorbed into systemic circulation to avoid enzymatic degradation in the gut and liver. Additionally, thin sublingual mucosa (about 190 μm compared to 500–800 μm of the buccal mucosa) and availability of plenty of blood supply at the sublingual region allows excellent drug penetration (absorption) to attain high plasma drug concentration with a rapid onset of action. A well-known example nitro-glycerine drug used for the treatment of acute angina (4). One problem related with sublingual drug delivery is the fact that the patient does have a tendency to involuntarily swallow liquids greater than 200 μL and rapid removal of drug owing to the flushing action of saliva. Because of the involuntary swallowing of the drug, it is removed from the sublingual cavity and enters the gastrointestinal tract. To overcome this disadvantage, dosage form is needed to be in contact with sublingual mucosa for prolonged time & this can be done by adhesion of the dosage form to the moist surface of mucosa and resistance to the flushing action of saliva. To avoid flushing action & to retain dosage form for long time, bioadhesive polymer, chitosan was used in formulations. Since NSD is a drug of potential interest but suffers from challenging problems like low aqueous solubility, an attempt was made to enhance the solubility using pullulan & PEG 4000. Pullulan is a non-ionic polysaccharide, having several advantages as a macromolecular drug carrier, highly water-soluble and non-toxic, multiple hydroxyl groups that