Abstract

In recent years, gastroretentive drug delivery system (GRDDS) has gained researcher’s interest in the field of oral drug delivery. Various GRDDS approaches can be utilized to retain the dosage forms in the stomach and to release the drug slowly for an extended period of time. GRDDS can be used to prolong the residence time of delivery system in the stomach. This results in targeting of drug release at a specific site for the systemic or local effects. GRDDS can be used to overcome challenges associated with conventional oral dosage forms and to release the drug at a specific absorption site to improve bioavailability of particular drug substance. The challenges include fast gastric emptying of the dosage form which results in the poor bioavailability of the drug. Prolongation of the retention of drugs in stomach those having low solubility at high intestinal pH improves the solubility of drugs. GRDDS has proved to be effective in systemic actions as well as in local actions to treat gastric or duodenal ulcers. Local activity in the upper part of the small intestine can be obtained by improving the residence time of delivery system in the stomach. The system is useful for drugs which are unstable in the intestine or having a low solubility/permeability in the small intestine. Various GRDDS approaches include high density (sinking) systems, low-density (floating systems), mucoadhesive, expandable, unfoldable, superporous hydrogel systems, and magnetic systems.

Highlights

  • Oral route is the most appropriate and preferred route for systemic or local delivery of any drug

  • Gastroretentive drug delivery system (GRDDS) have two main problems which are the short gastric retention time (GRT) of GRDDS in the stomach and unpredictable short gastric emptying time of the delivery system, which may lead to insufficient drug release from the dosage form in the absorption area which results in low efficacy of administered drug

  • Since the last few decades, different types of GRDDS approaches have been designed and developed. These approaches include: High density or sinking systems which can be retained in the basal part of the stomach [8] low density or floating systems that continue to float on gastric fluid [9,10]

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Summary

Introduction

Oral route is the most appropriate and preferred route for systemic or local delivery of any drug. 0–5 factors that affect the residence time of the delivery systems in the stomach are food intake and its nature, frequency of intake [23,24], density, size and shape of dosage forms [25,26], patient gender, age, sex, body mass index, and disease status of the individual person (i.e., Diabetes and Chrohn’s disease) [15,27,28] and drugs that have effects on gastrointestinal transit time such as anticholinergic drugs such as atropine or prokinetic agents such as metoclopramide and cisapride [29]. Dosage forms with low density than gastric contents can float on the surface, whereas high-density systems go down to the bottom of the stomach.

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