Abstract
In recent years, many attempts have been made to enhance the drug bioavailability and therapeutic effectiveness of oral dosage forms. In this context, various gastroretentive drug delivery systems (GRDDS) have been used to improve the therapeutic efficacy of drugs that have a narrow absorption window, are unstable at alkaline pH, are soluble in acidic conditions, and are active locally in the stomach. In this review, we discuss the physiological state of the stomach and various factors that affect GRDDS. Recently applied gastrointestinal technologies such as expandable, superporous hydrogel; bio/mucoadhesive, magnetic, ion-exchange resin; and low- and high-density-systems have also been examined along with their merits and demerits. The significance of in vitro and in vivo evaluation parameters of various GRDDS is summarized along with their applications. Moreover, future perspectives on this technology are discussed to minimize the gastric emptying rate in both the fasted and fed states. Overall, this review may inform and guide formulation scientists in designing the GRDDS.
Highlights
Oral drug delivery systems have dominated other drug delivery systems for human administration due to their various advantages including ease of administration, flexibility in formulation, cost-effectiveness, easy storage and transport, and high patient compliance
The main purpose of this review is to provide information on various gastroretentive drug delivery systems (GRDDS) that have been developed to date, as well as the physiological state of the stomach, suitable drug candidates for GRDDS, factors affecting GRDDS, and in vitro and in vivo characterization of GRDDS
Viscosity of polymer affects the consistency of the dosage form upon contact with the gastric fluid
Summary
Oral drug delivery systems have dominated other drug delivery systems for human administration due to their various advantages including ease of administration, flexibility in formulation, cost-effectiveness, easy storage and transport, and high patient compliance. Oral drug delivery systems face challenges such as low bioavailability due to the heterogeneity of the gastrointestinal system, pH of the commensal flora, gastric retention time of the dosage form, surface area, and enzymatic activity [1]. The failure of conventional drug delivery systems to retain drugs in the stomach may lead to the development of GRDDS. These systems offer several benefits such as prolonged gastric residence time (GRT) of dosage forms in the stomach up to several hours, increased therapeutic efficacy of drugs by improving drug absorption, and suitability for targeted delivery in the stomach. GRDDS can enhance the controlled delivery of drugs by continuously releasing the drug for an extended period at the desired rate and to the desired absorption site until the drug is completely released from the dosage form [1,2]
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