Revue de Pharmacovigilance

Abstrait

Design and Evaluation of a Controlled Release Drug Delivery System for Management of Rheumatism

Santhosh Kumar, Anusha G, Rajyalaxmi, Srinivas and Manoj

The present research was aimed to design, formulate and evaluate Mucoadhesive colon targeted microspheres of Ketoprofen for many advantages especially increased bioavailability and reduction in dosing frequency etc. Ketoprofen is a NSAID, like other drugs in this group reduces pain, inflammation and stiffness in rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. In this study an attempt was made to prepare mucoadhesive microspheres of Ketoprofen using the natural polymers designed for oral controlled release.

Ketoprofen microspheres were prepared following 32 full factorial designs with varying concentrations of the polymers using sodium alginate and natural polymer such guar gum, xanthan gum by orifice-ionic gelation method. The prepared ketoprofen microspheres were evaluated for surface morphology and particle shape, rheological studies. Micro encapsulation efficiency, swelling index and in vitro drug release studies were done, and compatibility studies. The microspheres were found discrete, spherical and free flowing.

The percentage yield ranged from 88% to 96% and encapsulation efficiency was from 86.23% to 94.46%. The particle size was found to be between 400-550 μm. From the in vitro drug release studies the (KPN5) showed 92.12% drug release in 12 hrs and showed better control of drug release. The in vitro release data was treated with mathematical equations, and was concluded that ketoprofen followed zero order release from the microspheres and Peppas model with non-Fickian diffusion Super Case II transport. The results indicate that Enteric coated mucoadhesive colon targeted microspheres of ketoprofen containing xanthan gum; guar gum provides a better option for controlled release action and improved bioavailability.