Yun Zhou1,
Min-Li Zhang1,
Bai-Jing Yuan1,
Jin-qi Yuan1,
Xin-Fang Zhao1,
Li Zhao2,
Hong-Qiang Ren3 
For correspondence:- Hong-Qiang Ren Email: renhongqiang256@hotmail.com Tel:+869932860314
Received: 3 September 2016 Accepted: 6 May 2017 Published: 29 June 2017
Citation: Zhou Y, Zhang M, Yuan B, Yuan J, Zhao X, Zhao L, et al. Herbal carrier-based floating microparticles of diltiazem hydrochloride for improved cardiac activity. Trop J Pharm Res 2017; 16(6):1239-1244 doi: 10.4314/tjpr.v16i6.5
© 2017 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..
Purpose: To formulate and characterize a gastroretentive floating drug delivery system for diltiazem hydrochloride using psyllium husk and sodium alginate as natural herbal carriers to improve the therapeutic effect of the drug in cardiac patients.
Methods: Floating microparticles containing diltiazem hydrochloride were prepared by the orifice ionic gelation technique. Various physicochemical properties of the floating microspheres were characterized, including drug content, particle size, surface morphology, in vitro drug release, and in vivo antihypertensive effect.
Results: The diltiazem hydrochloride microparticles exhibited a high drug content ranging from 63.23 ± 1.14 to 85.56 % ± 1.14 %. The particle size was 891.40 ± 2.14, 928.40 ± 1.79, 900.65 ± 2.22, and 1345.40 ± 1.36 μm (p < 0.05 compared to blank microspheres for formulations FDD1, FDD2, FDD3, and FFD4), respectively. Scanning electron microscopy showed that all the formulations had a smooth spherical surface with little pores and few cracks. The maximum floatability value was 83.11 % ± 3.18 % for FDD1. All of the formulations showed good in vitro drug release profiles, with a maximum release of 87.4 % of the drug at the end of 12 hours. The in vivo antihypertensive effects of the microparticles in human subjects were significant (p < 0.05 compared to normal controls), with a reduction in diastolic blood pressure from 120 to 78 mmHg at the end of 4 hours compared to diltiazem sustained-release tablets.
Conclusion: Psyllium husk and sodium alginate-based microspheres can be suitably prepared for the controlled delivery of diltiazem hydrochloride to cardiac patients. However, further study is required to develop the delivery system.
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