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Abstract

ABSTRACT:In this present research work, the aim was to develop ileocolonic targeted mini-tablets filled capsule system of flurbiprofen for treatment of rheumatoid arthritis. In the present study pH independent colon targeted system was developed and evaluated. SMEDDs of poorly water soluble drug flurbiprofen were prepared to enhance its dissolution rate and bioavailability. Mini-tablets of flurbiprofen were also prepared and filled in capsule. This capsule was coated with ethyl cellulose. Based on in-vitro dissolution studies it was noted that ethyl cellulose release takes place in colon (colon targeted). The design of formulation hence ensured colon targeted delivery of drug preventing premature drug release in stomach or small intestine and enhanced dissolution rate for enhancement of bioavailability. In vitro release studies were carried out in 0.1 N HCl pH 1.2, phosphate buffer pH 7.4 and phosphate buffer pH 6.8 mimicking in-vivo conditions for dissolution. SMEDDS exhibited a considerable increase in solubility of flurbiprofen and selected colon targeted formulation of pure drug successfully achieved colonic release of flurbiprofen with a lag time of 6 h and subsequent 75.895 % cumulative release in 11 h. Use of ethyl cellulose coated capsule efficiently delivers drug in colonic region without getting affected the SMEDDs inside for improving solubility and dissolution of drug. Thus, it was concluded that a novel ileo-colonic targeted delivery system of flurbiprofen filled by self micro emulsifying drug delivery system can be a better option for targeting early morning peak symptoms of rheumatoid arthritis and also to minimize the ulcers caused by side effects of flurbiprofen thus eliminating the use of proton pump inhibitors.

Design of Targeted Flurbiprofen Biomimetic Nanoparticles for Management of Arthritis: In Vitro and In Vivo Appraisal

“…It acts by inhibiting the COX-2 enzyme resulting in the suppression of the production of prostaglandin and consequently reducing inflammation and pain [13]. According to the Biopharmaceutical classification system, FLUR belongs to class II, which is characterized by poor water solubility and high permeability [14]. It has a short half-life (around four hours) thus, it is given orally in different doses (50-75 mg) three or four times daily to achieve the required therapeutic concentration [15].…”