Progress in Controlled Gastroretentive Delivery Systems

Abstract

Controlled release (CR) dosage forms have been extensively used to improve therapy with several important drugs. However, the development processes are faced with several physiological difficulties such as the inability to restrain and localize the system within the desired region of the gastrointestinal tract and the highly variable nature of the gastric emptying process. This variability may lead to unpredictable bioavailability and times to achieve peak plasma levels. On the other hand, incorporation of the drug in a controlled release gastroretentive dosage forms (CR-GRDF) which can remain in the gastric region for several hours would significantly prolong the gastric residence time of drugs and improve bioavailability, reduce drug waste, and enhance the solubility of drugs that are less soluble in high pH environment. Gastroretention would also facilitate local drug delivery to the stomach and proximal small intestine. Thus, gastroretention could help to provide greater availability of new products and consequently improved therapeutic activity and substantial benefits to patients. Controlled gastric retention of solid dosage form may be achieved by the mechanisms of floatation, mucoadhesion, sedimentation, expansion or by a modified shaped system. The purpose of this paper is to review the recent literature and current technology used in the development of gastroretentive dosage forms.

Gastroretentive microparticles for drug delivery applications

“…The systems absorb gastric fluid, on contact, swell and form a colloidal gel barrier (Sheth and Tossounian, 1979), that limits the rate of fluid absorption into the device and subsequently drug release (Sheth and Tossounian, 1984 (Garg and Gupta, 2008).…”

“…Other floating formulations include those using a combination of sodium alginate and sodium bicarbonate ; floating mini-capsules consisting a core of sodium bicarbonate, lactose and polyvinyl-pyrrolidone, coated with HPMC and systems produced using ion exchange resin technology (Garg and Gupta, 2008).…”

“…Floating systems can be divided into two categories: -gas generating systems and non-effervescent systems (Garg and Gupta, 2008).…”

Crushed Puffed Rice-HPMC-Chitosan based Single-Unit Hydro-dynamically Balanced System for the Sustained Stomach Specific Delivery of Metoprolol Succinate

“…The gel strength is also a rate-limiting step for the sustaining of drug (Soni et al, 2016). The gel strength can be increased by increasing the viscosity and this is achieved by the changing in the grades, addition with some another polymer or change in the concentration (Bernkop-Schnürch et al, 2012;Garg et al, 2008;Boldhane et al, 2010). Selection of HPMC and HMWCH is based on the previously reported work by one of the authors of this study (Soni et al, 2016;Verma et al, 2017).…”

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“…[2] The goal of any drug delivery system is to provide a therapeutic amount of the drug to the proper site in the body to achieve promptly, and then maintain, the desired drug concentration, to ensure the safety of drugs as well as patient compliance which is not achieved by conventional oral drug delivery. [3] Hence, there is need of controlled release drug delivery systems to overcome this problem.…”