International Journal of Drug Delivery 6 (2014) 121-132 http://www.arjournals.org/index.php/ijdd/index Original Research Article Preparation and evaluation of oral controlled release mucoadhesive microspheres of Ketorolac tromethamine Potu Appa Rao 1 , Prabhakar Reddy Veera Reddy 2 *Corresponding author: Potu Appa Rao 1 Balaji Institute of Pharmacy, Narsampet, Warangal, Andhra Pradesh-506331, India. 2 College of Pharmacy, Palamuru University, Mehabub Nagar-AP, Andhra Pradesh- India. Abstract Recently, lot of emphasis is being laid on oral controlled release multiple unit particulate (MUP) dosage forms, for their significant and potential benefits. Ketorolac tromethamine (KTM) is a potent non-narcotic analgesic and anti-inflamatory drug administered orally in multiple divided doses (10 mg four times a day) for the management of mild to moderate post-operative pain. KTMÊs short biological half-life demands frequent administration of the drug leading to poor patient compliance and inadequate pain management. Hence, the present investigation was undertaken to develop and evaluate oral controlled release mucoadhesive microspheres by ionotropic gelation method using natural and biodegradable polymers such as sodium carboxy methyl cellulose (Na CMC) and sodium alginate (SA). The influence of various formulation factors on the drug entrapment efficiency, in vitro drug release, micromeritic properties, and mucoadhesion ability was investigated. Scanning electron micrographs of alginate beads loaded with drug exhibited rough surface morphology and sizes were found to be in the range of 842 to 1265 øm. Among all the formulations, the drug loaded microspheres of formulation CA6 showed the highest drug release retarding effect over a period of 8 hours. The drug-polymer compatibility studies and solid state properties were investigated by Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) X- Ray diffraction techniques (X-RD). Keywords: Microspheres, Ketorolac tromethamine, controlled release, Ionotropic gelation technique, FTIR. Introduction Single-unit CR delivery systems or monolithic systems, generally may suffer from certain disadvantages such as unintentional disintegration of the formulation due to technological deficiency or abnormal or unusual gastric physiology leading to drastic changes in some patients.[1] Multi-particulate drug delivery systems contain a multiplicity of small individual units, each capable of exhibiting required characteristics. These systems, consists of thousands of spherical particles with diameter of 0.05-2.00mm.[2] MUPs offer all the advantages of a single unit formulations yet devoid of the dangers of alteration in a drug release profile and formulation behavior due to unit to unit variation, change in gastro-luminal pH and enzyme population. Such benefits can lead to increased bioavailability, less risk of systemic toxicity, reduced risk of local irritation, and predictable gastric emptying. MUPs.[3] These drug delivery systems, because of the smaller particle size, are able to pass through the gastrointestinal (GI) tract easily, leading to less inter- and intra-subject variability and dispersed more uniformly along the GI tract and result in more uniform drug absorption. The significant increase in the surface area of the drug loaded microspheres will enhance the exposure of the drug to the absorption site thus increasing the over all absorption of drug.[4] Moreover, MUPs can exhibit better in vivo performance than a single-unit system, as they show less erratic gastrointestinal transit times and are more sparsely scattered over the intestinal tract, thus providing greater uniformity of drug absorption, reduced potential for mucosal irritation and provide more reproducible drug release.[5] With these systems, even the safety profile the drug could be improved, mainly because the release characteristics are built into each sub unit.[6] These subunits units can either be filled into a sachet and encapsulated or compressed into a tablet. Numerous hydrophilic polymers, and in particular, polysaccharides, as well as their derivatives, have been employed in the formulation of modified-release dosage forms.[7] Recently, alginate beads containing several substances have been prepared by the gelation of alginate with calcium cations and the behaviour of the release of these substances has been investigated.[8] Alginic acid is a linear block polysaccharide copolymer made of β- D-mannuronic acid (M) and -L-guluronic acid (G) residues joined by 1,4 glycosidic linkages,and derived from sea weed. ISSN: 0975-0215 This work is licensed under a Creative Commons Attribution 3.0 License . CORE Metadata, citation and similar papers at core.ac.uk Provided by Advanced Research Journals