Original Article FORMULATION AND EVALUATION OF FLOATING-MUCOADHESIVE MICROSPHERES OF NOVEL NATURAL POLYSACCHARIDE FOR SITE SPECIFIC DELIVERY OF RANITIDINE HYDROCHLORIDE VIKRAM KUMAR SAHU 1* , NITIN SHARMA 2 , PRATAP KUMAR SAHU 3 , SHUBHINI A. SARAF 4 1 Department of Pharmacy, Maharana Pratap College of Pharmacy, Kanpur, 209217, India, 2 Meerut Institute of Engineering and Technology, NH-58, Baghpat Crossing, Partapur Bypass Road, Meerut, 250005, India, 3 School of Pharmaceutical Sciences, Siksha 'O' Anusandhan University, Bhubaneswar, 751030, India, 4 Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University, Lucknow, 226025, India Email: vikramsahuknp@gmail.com Received: 12 Nov 2016, Revised and Accepted: 17 Apr 2017 ABSTRACT Objective: Localization of ranitidine hydrochloride (RH) into the upper part of the intestinal tract is beneficial for better drug bioavailability. Present work described the method of preparation of novel plant polysaccharide based floating microspheres for delivery of the drug into the stomach. Methods: Polysaccharide was extracted from the seeds of plant Tamarindus indica (TI). Extracted polysaccharide was evaluated for some physicochemical parameters. Floating-mucoadhesive microspheres were prepared by using extracted polysaccharide as mucoadhesive excipients while eudragit as a release controlling polymers by using emulsion crosslinking method. Chemical crosslinking was done by using epichlorohydrin. Prepared microspheres were evaluated for their drug-polymer compatibility study by using fourier transform infrared spectroscopy (FT-IR). Further characterization such as size, surface properties, swelling index, percentage encapsulation, in vitro buoyancy and drug release was performed. Results: FT-IR study confirms the chemical crosslinking of extracted polysaccharide and also drug stability during processing of microspheres. The size of microspheres was in the range of 5.38 to 7.84 µm. SEM images revealed that all batches were of spherical in size and smooth surface. The swelling index showed better swelling in the range of 158-257 percentages. Encapsulation efficiency was found to be decreased by decreasing the concentration of polysaccharide. In vitro buoyancy study possesses that formulation F1 showed better floating ability as compared to the others. Finally, in vitro drug release study revealed that prepared microspheres were able to release the 100% drug within 8-12 h, indicating sustain release behavior. Conclusion: Present study concludes that polysaccharide of TI may be used as excipients for the preparation of floating-mucoadhesive microspheres. Keywords: Tamarindus indica, Ranitidine hydrochloride, Floating microspheres, Natural polymer © 2017 The Authors. Published by Innovare Academic Sciences Pvt Ltd. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/) DOI: http://dx.doi.org/10.22159/ijap.2017v9i3.16137 INTRODUCTION RH is a commonly used antacid as H2 The floating system is used for localized drug release into the specific region of the gastrointestinal tract (GIT). This system can be effervescent or non-effervescent depends on ingredients used in the delivery system. The most commonly used excipients in non- effervescent floating drug delivery system are either swellable or gel forming hydrocolloids and polysaccharide. These systems are also known as plug type system due to the tendency to remain lodged near the pyrrolic sphincter [3]. Nowadays, a large number of plant polysaccharide has been investigated for their potential role in the floating drug delivery system. These polymers have a tendency to swell on gastric media and float, therefore, increasing the residential time of formulation into the upper part of GIT. Additionally, this plant polysaccharide has some advantages such as biodegradable, biocompatible, low cost and relatively free availability [4]. receptor antagonist which shows maximum absorption at the initial part of small intestine. Moreover, colonic metabolism is also responsible for poor oral drug bioavailability [1]. Effective treatment can be achieved by administration of 200 mg of RH, three times a day, which leads to a patient in compliance. In order to improve therapeutic action and patient compliance, it is required to design a formulation which can increase the retention of the drug into the upper part of along with sustain release action up to 12 h [2]. With the same context, in the present work drug loaded floating mucoadhesive microspheres were developed to improve the residential time of RH into upper GIT. A novel plant polysaccharide was investigated for their application in the mucoadhesive delivery system. The polysaccharide was isolated from the seeds of TI. The polysaccharide of TI is nonionic, neutral, branched structure consist of cellulose like backbone which carries xylose and galactoxylose subunits. Polysaccharide has been investigated for many applications such as gelling agent, tablet binder, stabilizer and thickening agent [5, 6]. So far, the polysaccharide is not evaluated in the floating drug delivery system. Aim of present work was to investigate the role of novel TI polysaccharide in development of floating mucoadhesive microspheres for localized drug delivery of RH specifically into upper parts of GIT. MATERIALS AND METHODS RH was obtained as generous gift sample from Hetero labs, Hyderabad, India. Seeds of TI were purchased from local market of Kanpur (UP). All other materials such as Eudragit, castor oil, epicholorhydrin, and sodium bicarbonate were of analytical grade and were procured from commercial sources. Polysaccharide extraction TI polysaccharide was extracted as per reported methods in various publications [7]. The seed were process by separating the brown peels from the kernel seed with the blender and plastic sieve were used to separate the seed. The seed were powdered and boiled with distilled water. Mucilaginous juice was separated by filtration through muslin cloth under vacuum and precipitated by ethanol. Precipitate was dried at 50 °C for 2 d. Further, the extracted dry polysaccharide was characterised in terms of purity and viscosity. International Journal of Applied Pharmaceutics ISSN- 0975-7058 Vol 9, Issue 3, 2017