ANTIEPILEPTIC RECTAL HYDROGEL LOADED WITH CARBAMAZEPINE – RICE BRAN WAX MICROSPHERES

Abstract

ABSTRACTObjectives: The objective behind the study is to develop a mucoadhesive rectal hydrogel from carbamazepine (CBZ) – rice bran wax (RBW)microspheres for the purpose of controlled release for the treatment of epilepsy.Methods: The study was conducted to formulate controlled release rectal hydrogel loaded with CBZ – RBW microspheres in two different natural polymers,RBW and collagen which are prepared by modified cooling induced solidification method and gel preparation along with their evaluation studies.Results: A thorough analysis of the optimized gel revealed that all the evaluation parameters evaluated are within the acceptable limits. Further, theoptimized microsphere formulation (M5) was used to formulate it as rectal hydrogel using polymer collagen and was characterized. The mucoadhesiontime of 25% w/w collagen hydrogel (H4) was 565 minutes, allowing the loaded microspheres to be attached on rectal mucosa. In vitro drug releasefrom the mucoadhesive hydrogel formulations showed controlled drug release pattern with a maximum drug release of 96.45±0.35% for optimizedH4 formulation after 12 hr, followed zero order release pattern with diffusion mediated Higuchi model. Ex vivo permeation studies using bovine rectalmucosa revealed that H4 formulation showed greater permeability compared to control. Histopathological findings revealed that H4 formulation issafer for rectal administration without any signs of rectal irritancy. The stability studies of optimized formulation (H4) proved that hydrogel remainedstable over a wide range of temperature condition.Conclusion: Hence, the developed rectal hydrogel formulation seems to be a viable alternative to conventional drug delivery system for the effectivemanagement of epilepsy.Keywords: Carbamazepine, Rice bran wax, Rectal hydrogel, Sustainability.