Abstract
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.Keywords: Diltiazem, Cardiac disease, Psyllium husk, Sodium alginate, Microsphere, Microparticle, Controlled drug release, Gastroretentive, Floating drug delivery
Highlights
Herbal-based drug delivery systems have long been used in folk medicine, and herbal medicines of natural origin show good therapeutic activity with minimal side effects
It forms a gel upon contact with water, and its swelling behavior makes it suitable for use as a carrier for diltiazem hydrochloride (HCl) microparticles [7,8]
The mean particle size varied significantly according to the different proportions of polymers used, which may have been due to differences in the viscosity of the polymer solution [16,17,18,19,20]
Summary
Herbal-based drug delivery systems have long been used in folk medicine, and herbal medicines of natural origin show good therapeutic activity with minimal side effects. Psyllium husk is a source of mucilaginous fiber obtained from the dried seed coats of Plantago ovata. It forms a gel upon contact with water, and its swelling behavior makes it suitable for use as a carrier for diltiazem hydrochloride (HCl) microparticles [7,8]. Diltiazem HCl is a calcium channel blocker that inhibits the influx of calcium (Ca2+) ions during membrane depolarization in cardiac and vascular smooth muscle It is effective in the treatment of hypertension and angina pectoris due to its cardiac effects. The present study was performed to develop a gastroretentive floating drug delivery system for diltiazem HCl using psyllium husk and sodium alginate as natural herbal carriers to achieve improved therapeutic effects in cardiac patients. The samples were withdrawn, filtered, diluted appropriately, and measured spectrophotometrically at 243 nm to determine the drug content
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