Formulation and Evaluation of Gastroretentive Floating Microspheres of Amiloride Hydrochloride

Authors

  • Suraj Kumar Department of Pharmaceutics, University of Uttarakhand Technical University, Dehradun, Uttarakhand, India.
  • Bishnu Upreti Department of Pharmaceutics, University of Uttarakhand Technical University, Dehradun, Uttarakhand, India.

DOI:

https://doi.org/10.21276/apjhs.2024.11.3.04

Keywords:

Amiloride HCL, Floating microspheres, Hydroxypropyl methylcellulose k-100

Abstract

Background: Amiloride, a potassium-sparing diuretic, is widely prescribed for the management of hypertension, congestive heart failure, and various renal disorders. However, its low oral bioavailability due to extensive first-pass metabolism and short half-life necessitates frequent dosing, leading to patient inconvenience and compromised therapeutic outcomes. To address these limitations, the development of novel drug delivery systems capable of enhanced gastrointestinal retention of amiloride has garnered significant attention. Among these, gastroretentive microspheres represent a promising approach, offering prolonged drug release and improved absorption. Objectives: The present work by formulation and evaluation of gastroretentive floating microsphere (FM) plays a highly significant role as a particulate drug delivery method. Particle sizes for microspheres range from 0.1 to 200 μm, and they can be administered orally, parenterally, nasally, ophthalmologically, transdermal, colonically, etc. Site-specific targeting and enhanced release kinetics are just two of the issues that have been solved through recent advances in microspheres, including those that are mucoadhesive, hollow, floating, micro-balloons, and magnetic. Microspheres will play a key role in novel drug delivery in the future by fusing different new methods, particularly sick cell sorting, genetic materials, safe, targeted, and effective drug delivery. Discussion: Hydroxypropyl methylcellulose (HPMC), polyvinylpyrrolidone, and ethylcellulose were used in varying concentrations to give the FMs of amiloride HCl release-controlling properties by increasing their bioavailability. Lactose was used as a diluent and sodium bicarbonate served as an effervescent agent. Using a solvent evaporation method approach, the gastroretentive FM of amiloride HCl was created. The generated microsphere indicated good floating strength and remained buoyant in the sustained released medium for 24 h. For systemic delivery of amiloride, a potassium-sparing diuretic and antihypertensive medication, through the oral route, a gastroretentive FMs drug delivery system was developed. The different ratios of ethylcellulose and HPMC K-100, sodium lauryl sulfate, sodium bicarbonate, and ethanol are used in formulation. The weight, thickness, percentage of moisture absorbed and lost, surface pH, folding resistance, content homogeneity, in vitro residence time, in vitro release, and ex vivo penetration of the microspheres were all assessed. Conclusion: The formulation and evaluation of gastroretentive FMs represent a significant advancement in particulate drug delivery systems. These microspheres, with particle sizes ranging from 0.1 to 200 μm, offer versatility in administration.

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Published

2024-11-14

How to Cite

Suraj Kumar, & Bishnu Upreti. (2024). Formulation and Evaluation of Gastroretentive Floating Microspheres of Amiloride Hydrochloride. Asian Pacific Journal of Health Sciences, 11(3), 14–24. https://doi.org/10.21276/apjhs.2024.11.3.04