Abstract

Ms. Shramika A. Chore*, Dr. S. J. Dighade, Prof. Sanjeevani S. Deshkar and Ms. Seema S. Borkar

ABSTRACT

The rectum has been an accepted site of drug delivery. Its principal applications have been for local therapy. Some populations are less willing to accept this route as a standard method for drug delivery, but it is the most easily accessible area of the lower GI tract.[1,3] Diclofenac sodium is the most popular NSAIDs have a relatively high therapeutic index in comparison to other NSAIDs. Its half-life is 2 hours. It is a non-steroidal anti- inflammatory drug (NSAID) with analgesic and antipyretic properties. Diclofenac is used to treat pain, dysmenorrhea, ocular inflammation, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and actinic keratosis. In the present study, various in situ gelling rectal formulations using Poloxamer 407 with and without microemulsions were prepared. Different formulations of Diclofenac sodium using Poloxamer 407 in concentration of 15-20% w/w (B1-B10) were prepared with and without microemulsion addition. Further, different formulations of poloxamer 407 (18%w/w) were also prepared by combining with HEC in concentration of 0.5 %w/w (B13) and HPMC E50 LV in concentration of 0.5 %w/w (B14). All these rectal formulations were evaluated for appearance, clarity, pH, gelling ability, viscosity and percent drug release. The formulations showing transparent and clear appearance, quick and stable gelation, shear thinning properties, excellent sustained drug release up to 82- 98% after 8hrs were selected for further characterization. The selected formulations were then subjected for studying the stability to refrigerated condition (5°±3). The optimized formulations, B4 (18%w/w poloxamer with drug microemulsion), B13 (18%w/w poloxamer, 0.5 %w/w HEC and drug microemulsion) and B14 (18%w/w poloxamer, 0.5 %w/w HPMC E50 LV and drug microemulsion) were found to be very clear, transparent, forming quick and stable gels with shear thinning behavior. The optimized formulations B4, B13 and B14 showed excellent mucoadhesion and sustained drug release.