Devang Sarvaiya, Ujwala Shinde, Pankaj Jain, Sadhana Sathaye1
1Department of Pharmaceutics, Bombay College of Pharmacy, Santacruz, Kalina, Mumbai, 2Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Matunga, Mumbai, India
E-mail: ddsarvaiya@gmail.com
Background: The present research work was aimed at preparing microspheres for oral delivery of bromelain, an anti-inflammatory enzyme from pineapple fruit (Ananas comosus). Objective: The objective was to improve the oral delivery of this proteolytic enzyme by circumventing its instability in acidic environment and modulating its release in intestine for its anti-inflammatory action. Materials and Methods: Sodium alginate, calcium chloride, bromelain. Microspheres were prepared by ionotropic gelatin technique dropping the sodium alginate solution to magnetically stirred calcium chloride solution. Results: Optimized batch of microspheres were prepared using 3% sodium alginate concentration, 0.05M calcium chloride and curing time of 20 min with highest entrapment efficiency of 69.98%± 0.087%. In vitro release studies showed very low amount of drug release in 0.1N HCl and sustained release in simulated intestinal fluid pH 6.8 with more than 90% drug release at the end of 2 hrs. The drug release profiles for the optimized batch was best fitted with Korsmeyer-Peppas as well as Higuchi model based on regression coefficients. Bromelain microspheres showed 62.90%±1.44% edema inhibition in rat paw edema model in comparison to marketed bromelain formulation which showed 69.35% ±1.44% inhibition at end of 2 hrs. Optimized batch of microspheres were found to be stable as per ICH guidelines of stability. Conclusion: Thus alginate based microsphere drug delivery system can be effectively developed for oral delivery of bromelain and can be considered as an alternative approach to conventional NSAIDs and side effects associated with it.
