FORMULATION AND IN VITRO EVALUATION OF RAMELTEON TABLETS FOR COLON DRUG DELIVERY SYSTEM BY COMPRESSION COATING

Objective: Ramelteon, is a sleep agent that selectively binds to the MT1 and MT2 receptors in the suprachiasmatic nucleus (SCN), instead of binding to GABAA receptors. In the present research work, the formulation of ramelteon targeted to colon by using various polymers developed. Methods: Colon-targeted tablets were prepared in two steps. Initially, core tablets were prepared and then the tablets were coated by using different pH dependent polymers. Ethylcellulose, Eudragit RLPO and L100 were used as enteric coating polymers. The precompression blend of all formulations was subjected to various flow property tests and all the formulations were passed the tests. The tablets were coated by using polymers and the coated tablets were subjected to physical characterization, drug content, in vitro drug release and kinetics of drug release. Results: Among all the formulations, F4 formulation was found to be optimized as it was retarded the drug release up to 18 h and showed maximum of 99.25% drug release. It followed the first-order kinetics mechanism. All the formulations having Korsmeyer-Peppas ‘n’ values are in the range of 0.540 to 0.818. Hence, it was concluded that the prepared formulations followed non-Fickian diffusion. Conclusion: An effective and stable remelteon colon targeted formulation developed for treating insomnia.

Recent Advances in Colon Drug Delivery Technology.

: Colon targeted drug delivery technology; an approach of immense potential has acquired tremendous significance for managing a number of ailments particularly of colon and for delivering therapeutic proteins and peptides systemically. The major hurdles for delivering drug in colonic region include absorption and degradation pathways in the upper gastrointestinal tract (GIT). To achieve a triumphant colonic delivery, therapeutic agent must be sheltered from getting absorbed in the preliminary region of GIT, in addition, ensure its release in proximal colon in a controlled way. The principle approaches for instance prodrug approach, pH sensitivity, time-dependency (lag time), degradation by microbes etc. have been effectively applied for obtaining colon targeted drug delivery. These approaches have accomplished immense relevance. Therefore, incessant attempts have been mainly focused on the design of colon targeted drug delivery systems having enhanced site specificity along with study of its versatile drug release kinetics to achieve diverse therapeutic requirements. The current manuscript illustrates significance of different colon drug delivery systems and general considerations for designing colon targeting systems including primary as well as novel approaches. Recent investigational studies carried out by scientific communities worldwide for the designing and preparation of various colon targeted formulations along with their significant insights have been described. Recent patents, structure property relationship and dissolution aspects pertaining to the colon specific drug delivery have also been depicted.

Nanoparticles as Budding Trends in Colon Drug Delivery for the Management of Ulcerative Colitis

Inflammatory Bowel Disease (IBD) is a disorder of the gastrointestinal tract, which is characterized by Crohn’s disease and Ulcerative colitis. Ulcerative colitis (UC) is a chronic idiopathic relapsing colon disease distinguishes by the interference of epithelial wall and colonic site tenderness. For the treatment of ulcerative colitis, various side effects have been reported, due to the non-specific delivery of the targeted drug of the conventional system. This review will explain the reader about various considerations for the preparation of orally administered NPs drug delivery systems for the treatment of ulcerative colitis. Moreover, principles and novel strategies for colon targeting based on the physiology of colon so that the tract of gastro intestine can be used as the identification marker for a target site for drugs. Besides this, the role of phytomedicines in controlling and managing the ulcerative colitis has been discussed. Additionally, the major problem for the smart delivery of NPs in clinical applications with their difficulties in Intellectual Property Rights (IPR) was also discussed. Finally, this review provides various potential approaches to NPs for the treatment of UC.

Formulation and evaluation of deflazacort loaded mucoadhesive microsphere for colon drug delivery system

Irritable bowel disease is very common colon disease. Deflazacort is one of the best drug with clinical activity against Irritable bowel disease. Microsphere system are effectively protect drugs against premature degradation, to localize drug molecules at the target site of action and to control the time and rate of release. Mucoadhesive microspheres enhance the bioavailability of orally given drugs by lengthened contact time of drug with the intestinal mucosa. The main disadvantage of these microspheres is adherence to the substrate by non-specific interaction. To overcome this limitation, microspheres are prepared by emulsification method to treat irritable bowel disease. Chitosan microspheres were prepared by Ionotropic Gelation method. Microspheres were coated with Eudragil S using solvent evaporation method. Keywords: Deflazacort, Mucoadhesive, Microspheres, Irritable bowel disease

A Micellar-Hydrogel Nanogrid from a UV Crosslinked Inulin Derivative for the Simultaneous Delivery of Hydrophobic and Hydrophilic Drugs

Hydrogels are among the most common materials used in drug delivery, as polymeric micelles are too. They, preferentially, load hydrophilic and hydrophobic drugs, respectively. In this paper, we thought to combine the favorable behaviors of both hydrogels and polymeric micelles with the specific aim of delivering hydrophilic and hydrophobic drugs for dual delivery in combination therapy, in particular for colon drug delivery. Thus, we developed a hydrogel by UV crosslinking of a methacrylated (MA) amphiphilic derivative from inulin (INU) (as known INU is specifically degraded into the colon) and vitamin E (VITE), called INVITEMA. The methacrylated micelles were physicochemically characterized and subjected to UV irradiation to form what we called the “nanogrids”. The INVITEMA nanogrids were characterized by DSC, SEM, TEM, water uptake and beclomethasone dipropionate (BDP) release. In particular, the release of the hydrophobic drug was specifically assessed to verify that it can spread along the hydrophilic portions and, therefore, effectively released. These systems can open new pharmaceutical applications for known hydrogels or micelle systems, considering that in literature only few examples are present.