Floating Microparticulate Oral Diltiazem Hydrochloride Delivery System for Improved Delivery to Heart
Purpose: To formulate and evaluate floating microparticulate oral diltiazem delivery system for possible delivery to the heart.
Method: Floating microspheres were prepared using cellulose acetate and Eudragit RS100 polymers by emulsion solvent evaporation technique. The dried floating microspheres were evaluated for micromeritic properties (flow properties, density, particle size determination) scanning as well as by electron microscopy, and in vitro floatability and drug release studies.
Results: The microspheres showed good buoyancy, good flow properties (angle of repose ranging from 24.29 to 29.02 º), particle size (262.09 to 409.60 μm) and good drug loading (74.29 to 92.09 %). The microspheres were porous, hollow and spherical. All the formulations showed good in vitro controlled drug release in the range of 77.62 ± 2.12 to 97.50 ± 1.04 % at the end of 12 h. Drug release was diffusion-controlled and followed zero order kinetics.
Conclusion: Microparticulate floating (gastroretentive) oral drug delivery system of diltiazem prepared using cellulose acetate and Eudragit R5100 may be an effective alternative to conventional oral tablets for cardiac drug delivery.
Keywords: Cardiac, Microparticulate, Drug release, Gastroretentive, Floating microspheres, Diltiazem hydrochloride