Abstract

The purpose of writing this review on gastroretentive drug delivery systems (GRDDS) was to compile the recent literature with a special focus on various gastroretentive approaches that have recently become leading methodologies in the field of site-specific orally administered controlled release drug delivery. One of the complex processes in the human body is gastric emptying, as it is highly variable, which makes the in vivo performance of the drug delivery systems uncertain. GRDDS has gained immense popularity in the field of oral drug delivery recently. It is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with the conventional oral delivery system. Conventional drug delivery systems may not overcome the issues imposed by the gastrointestinal tract (GIT) such as incomplete release of drugs, decrease in dose effectiveness, and frequent dose requirement. To overcome this variability, a controlled drug delivery system with a prolonged gastric residence time of >12 h in the stomach can be of great practical importance for drugs with an absorption window in the upper small intestine. GRDFs enable prolonged and continuous release of the drug to the upper part of the GIT and thus significantly extend the duration of drug release and improve the bioavailability of drugs that have a narrow therapeutic window; by this way, they prolong dosing interval and increase compliance.

Highlights

  • Gastroretentive drug delivery system (GRRDS) Oral controlled-release (CR) dosage forms (DFs) were developed over the past three decades due to their therapeutic benefits, for example, ease of administration, patient compliance, and malleability to the formulation. This is due to several physiological difficulties such as the inability to bring under control and detect controlled drug delivery systems within the preferred region of the gastrointestinal tract (GIT) due to variable gastric emptying and motility Fig. 1

  • For more than half a century, pharmaceutical scientists have focused on the development of ideas to increase the gastric residence time of DFs [2]

  • During a state of fasting, cycling through the stomach and intestines, a series of electrical events occur every 2–3 h. This is called the Inter-Digestive Milo Electric Cycle or Migrating Milo Electric Cycle (MMC), which is divided into the following four steps described by Wilson and Washington (1989)

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Summary

INTRODUCTION

Gastroretentive drug delivery system (GRRDS) Oral controlled-release (CR) dosage forms (DFs) were developed over the past three decades due to their therapeutic benefits, for example, ease of administration, patient compliance, and malleability to the formulation This is due to several physiological difficulties such as the inability to bring under control and detect controlled drug delivery systems within the preferred region of the gastrointestinal tract (GIT) due to variable gastric emptying and motility Fig. 1. Prolonged gastric retention improves bioavailability, reduces residual waste, and increases the solubility of drugs soluble in the high pH environment of the GIT This includes applications for local delivery of the stomach and small intestine [4]

ANATOMY OF THE GIT
POTENTIAL DRUG CANDIDATES FOR GRDDS
BASIC GIT PHYSIOLOGY
FLOATING SYSTEMS
SWELLING AND EXPANDING SYSTEMS
INCORPORATION OF PASSAGE DELAYING FOOD AGENTS
ION EXCHANGE RESINS
OSMOTIC REGULATED SYSTEMS
FLOATING DRUG DELIVERY SYSTEMS
METHOD OF PREPARATION OF FLOATING MICROSPHERE
EMULSION SOLVENT EVAPORATION TECHNIQUE
Salt addition
Microsphere in an aqueous or organic phase
Molding Mechanical fragmentation
Heating and agitation Polymerization
Findings
CHARACTERIZATION OF GASTRORETENTIVE DFS
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