Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Floating microparticulate oral diltiazem hydrochloride delivery system for improved delivery to heart

Hai-feng Cheng¹, Yan Feng² , Qun-jun Duan¹, Da-Ming Jiang¹, Kai-Yu Tao¹

¹Department of Cardiovascular Surgery; ²Department of Cardiovascular Interventional Center, Second Affiliated Hospital Zhejiang University College of Medicine, Hangzhou 310009, China.

For correspondence:- Yan Feng Email: fengyan31900@gmail.com Tel:+8657187784704

Received: 12 February 2015 Accepted: 23 May 2015 Published: 29 June 2015

Citation: Cheng H, Feng Y, Duan Q, Jiang D, Tao K. Floating microparticulate oral diltiazem hydrochloride delivery system for improved delivery to heart. Trop J Pharm Res 2015; 14(6):935-940 doi: 10.4314/tjpr.v14i6.1

© 2015 The authors.
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Abstract

Purpose: To formulate and evaluate floating microparticulate oral diltiazem delivery system for possible delivery to the heart.

Methods: 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