Floating microspheres: a review

Jagtap Yogesh Mukund,Ranpise Nisharani Sudhakar,Bhujbal Rohan Kantilal

doi:10.1590/s1984-82502012000100003

Jagtap Yogesh Mukund, Ranpise Nisharani Sudhakar + Show 1 more

Open Access

https://doi.org/10.1590/s1984-82502012000100003

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Abstract

Gastric emptying is a complex process, one that is highly variable and that makes in vivo performance of drug delivery systems uncertain. A controlled drug delivery system with prolonged residence time in the stomach can be of great practical importance for drugs with an absorption window in the upper small intestine. The main limitations are attributed to the inter- and intra-subject variability of gastro-intestinal (GI) transit time and to the non-uniformity of drug absorption throughout the alimentary canal. Floating or hydrodynamically controlled drug delivery systems are useful in such applications. Various gastroretentive dosage forms are available, including tablets, capsules, pills, laminated films, floating microspheres, granules and powders. Floating microspheres have been gaining attention due to the uniform distribution of these multiple-unit dosage forms in the stomach, which results in more reproducible drug absorption and reduced risk of local irritation. Such systems have more advantages over the single-unit dosage forms. The present review briefly addresses the physiology of the gastric emptying process with respect to floating drug delivery systems. The purpose of this review is to bring together the recent literature with respect to the method of preparation, and various parameters affecting the performance and characterization of floating microspheres.

Highlights

Among the different routes of drug administration, the oral route has achieved the most attention, partly due to the ease of administration and to the important flexibility in dosage form design (Soppimath et al, 2001)
In most cases, the important variability of the gastrointestinal tract physiology and of its transit time leads to unpredictable bioavailability and non reproducible therapeutic effects
One requisite for the successful performance of oral controlled release drug delivery systems is that the drug should have good absorption throughout the gastrointestinal tract (GIT), preferably by passive diffusion (Patil et al, 2006)

Summary

INTRODUCTION

Among the different routes of drug administration, the oral route has achieved the most attention, partly due to the ease of administration and to the important flexibility in dosage form design (Soppimath et al, 2001). Several difficulties are faced in designing controlled release systems for better absorption and enhanced bioavailability One of such difficulties is the inability to confine the dosage form in the desired area of the gastrointestinal tract. Prolongation of gastric residence time (GRT) of a rate-controlled oral drug delivery system reduces inter-subject variability and the so-called “peak and valley” effect, leading to increased predictability and bioavailability of the dosage form, especially for molecules with a narrow absorption window. This is known as digestive motility pattern and comprises continuous contractions as in phase II of the fasted state These contractions result in reduced size of food particles (to less than 1 mm), which are propelled toward the pylorus in a suspension form. Reproducibility of the particle size of the formulation is the main problem associated with floating microspheres (Mitsutoshi et al, 2001)

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