Journal of Pharmaceutical Research And Opinion 1: 4 (2011) 108 - 112 Contents lists available at www.innovativejournal.in JOURNAL OF PHARMACEUTICAL RESEARCH AND OPINION Journal homepage: http://www.innovativejournal.in/index.php/jpro 108 RESEARCH FORMULATION AND EVALUATION OF COLON TARGETED CURCUMIN MICROSPHERES USING NATURAL POLYMERS Ankit Vajpayee * 1 , Suresh Fartyal 1 , Alok Pratap Singh 1 Sajal Kumar Jha 2 *1 NIMS Institute of Pharmacy, Jaipur, Rajasthan, India 2 Bengal College of Pharmaceutical Sciences & Research, Durgapur, India. ARTICLE INFO ABSTRACT Received 17 Jun 2011 Accepted 08 Sep 2011 Corresponding Author: Ankit Vajpayee NIMS Institute of Pharmacy, Jaipur (Rajasthan) Mobile Number :- +91 9413422666 vajpayee01@yahoo.com Curcumin is used to treat colon cancer, but it has very poor absorption in upper part of GIT. As a part of drug delivery, colon offers near neutral pH, reduced digestive enzymetic activity, a long transit time and increased responsiveness to absorption enhancers. The aim of present study is to identify suitable polymer (guar gum or xanthan gum) based microspheres promising in-vitro mouth-to-colon release profile. Curcumin loaded microspheres were prepared by ionic cross linking technique using calcium chloride. Three formulations with each polymer (sodium alginate: guar gum / sodium alginate: xanthan gum) using different concentrations were formulated by ionic cross linking technique. Microspheres were subjected to evaluation by studying parameters like percentage yield, particle size, IR spectroscopy, TLC, SEM, percentage entrapment efficiency and in-vitro release profile. In-vitro drug release study was performed using simulated gastric fluid and simulated intestinal fliud for 8 hrs. Natural or modified polysaccharides (guar gum, xanthan gum, locust gum, dextrans, starch, amylose, pectins) degraded by the human colonic flora, have thus been investigated as colonic drug delivery carriers. 0.75 percent polymer containing formulation showed retarded release at the end of 8 hrs. All the batches in first two hours showed very negligible release, then it showed increase in drug release up to 8 hours. Xanthan gum microspheres showed more retarded release than guar gum microspheres. The microspheres are spherical in shape and having rough surface. ©2011, JPRO, All Right Reserved. KeyWords: Colon Cancer, Curcumin Microspheres, Sodium Alginate, Guar Gum, Xanthan Gum INTRODUCTION Drug targeting to colon is useful when a delay in drug absorption is desired from the therapeutic point of view, such as treatment of diseases that have peak symptoms in the early morning, like nocturnal asthma, angina or arthritis 1 . By definition, an oral colonic delivery system should retard drug release in the stomach and small but allow complete release in the colon. The fact that such a system will be exposed to a diverse range of gastrointestinal conditions on passage through the gut makes colonic delivery via the oral route a challenging proposition. Targeted drug delivery to the colon would therefore ensure direct treatment at the disease site, lower dosing and fewer systemic side effects 2 . In recent times, colon-targeted drug delivery systems have gained importance for the systemic delivery of protein and peptide drugs 1 . Targeting of drugs to the colon via the oral route can be achieved by different approaches including different formulation systems, for which the drug release is controlled by different pH conditions, transit time, and intestinal microbial flora 3 . Various strategies have been developed to achieve colon targeting, such as, use of specific characteristics of the organ, for example, pH, microbial flora, enzymes, reducing medium, and transit time 4 . A number of serious diseases of the colon, for example, colorectal cancer, ulcerative colitis, and other inflammatory conditions could be treated more effectively if drugs are targeted to the colon 5-7 . The presence of certain enzymes in the colon, which have been involved to specifically cleave certain type of drugs attached to another molecule or a polymer, has been studied by a number of authors 8-10 . Colon cancer, one of the serious diseases, can also be treated by means of effective targeting of anticancer drugs to the colonic region 11 . Curcumin is the principal curcuminoid of the popular Indian curry spice turmeric. The curcuminoids are polyphenols and are responsible for the yellow color of turmeric. Curcumin is known for its antitumor, antioxidant, antiarthritic, anti-amyloid, anti-ischemic and anti- inflammatory properties. Its anticancer effects stem from its ability to induce apoptosis in cancer cells without