Special Issue "Gastro-retentive Dosage Forms: Concepts, Design, Testing and Manufacture"

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: closed (20 March 2019).

Special Issue Editors

Prof. Werner Weitschies
E-Mail Website
Guest Editor
Department of Biopharmacy and Pharmaceutical Technology, Institute of Pharmacy, University of Greifswald, Center of Drug Absorption and Transport, Felix-Hausdorff-Str. 3, D‐17487 Greifswald, Germany
Interests: Oral drug delivery; gastroretentive dosage forms; 3D printing; in vivo imaging of the GI tract; biorelevant in vitro tools; GI physiology
Dr. Mirko Koziolek
E-Mail Website
Guest Editor
Department of Biopharmacy and Pharmaceutical Technology, Institute of Pharmacy, University of Greifswald, Center of Drug Absorption and Transport, Felix-Hausdorff-Str. 3, D‐17487 Greifswald, Germany
Interests: Food effects; biorelevant in vitro testing; animal models; magnetic resonance imaging; human GI physiology; telemetric capsules

Special Issue Information

Dear Colleagues,

The gastric retention of a dosage form can offer enormous benefits with respect to oral pharmacotherapy and is particularly interesting for drugs with an absorption window in the upper small intestine, narrow therapeutic window and/or poor oral bioavailability. For these drugs, the extension of the gastric residence time may enable an increase in the oral bioavailability or an extension of the dosing interval. Moreover, peaks or fluctuations of the systemic drug concentration can be avoided by simultaneous controlled drug release. Therefore, different formulation concepts were developed in the past 40 years that guarantee reproducible retention in the stomach after oral intake. Most of these principles are based on flotation, mucoadhesion, sedimentation and expansion of the system by swelling or unfolding.

This Special Issue addresses novel strategies in the design, manufacturing and testing of gastroretentive dosage forms. Innovative concepts shall be presented that may overcome the current challenges of gastroretention. Furthermore, the development of gastroretentive drug delivery systems can only succeed if appropriate test methods are available early in development. Therefore, the focus will also be on the description of optimized in vitro and in vivo strategies for the testing of the gastroretentive dosage forms highlighted.

Prof. Werner Weitschies
Dr. Mirko Koziolek
Guest Editors

Manuscript Submission Information

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Keywords

  • Oral drug delivery
  • Gastroretentive dosage forms
  • Controlled drug delivery
  • Gastroretention
  • Stomach
  • Mucoadhesion
  • Expansion
  • Flotation
  • Swelling
  • Unfolding
  • Gastric emptying
  • GI physiology
  • Animal models
  • In vitro models

Published Papers (3 papers)

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Research

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Open AccessArticle
Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone
Pharmaceutics 2019, 11(6), 271; https://doi.org/10.3390/pharmaceutics11060271 - 10 Jun 2019
Abstract
In this study, we aimed to design a highly swellable and mechanically robust matrix tablet (SMT) as a gastroretentive drug-delivery system (GRDDS) capable of improving the dissolution behavior of β-lapachone with low aqueous solubility. For the preparation of SMTs, the cogrinding technique and [...] Read more.
In this study, we aimed to design a highly swellable and mechanically robust matrix tablet (SMT) as a gastroretentive drug-delivery system (GRDDS) capable of improving the dissolution behavior of β-lapachone with low aqueous solubility. For the preparation of SMTs, the cogrinding technique and freeze–thaw method were used to disperse β-lapachone in SMTs in an amorphous state and to enhance the swelling and mechanical properties of SMTs, respectively. As a result, the crystallinity of coground β-lapachone incorporated in the SMTs was found to be considerably decreased; thereby, the dissolution rates of the drug in a simulated gastric fluid could be substantially increased. The SMTs of β-lapachone also demonstrated significantly enhanced swelling and mechanical properties compared to those of a marketed product. The reason for this might be because the physically crosslinked polymeric networks with a porous structure that were formed in SMTs through the freeze–thaw method. In addition, β-lapachone was gradually released from the SMTs in 6 h. Therefore, SMTs of β-lapachone developed in this study could be used as GRDDS with appropriate swelling and mechanical properties for improving the dissolution behavior of hydrophobic drugs such as β-lapachone. Full article
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Review

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Open AccessReview
In Vitro and In Vivo Test Methods for the Evaluation of Gastroretentive Dosage Forms
Pharmaceutics 2019, 11(8), 416; https://doi.org/10.3390/pharmaceutics11080416 - 16 Aug 2019
Abstract
More than 50 years ago, the first concepts for gastroretentive drug delivery systems were developed. Despite extensive research in this field, there is no single formulation concept for which reliable gastroretention has been demonstrated under different prandial conditions. Thus, gastroretention remains the holy [...] Read more.
More than 50 years ago, the first concepts for gastroretentive drug delivery systems were developed. Despite extensive research in this field, there is no single formulation concept for which reliable gastroretention has been demonstrated under different prandial conditions. Thus, gastroretention remains the holy grail of oral drug delivery. One of the major reasons for the various setbacks in this field is the lack of predictive in vitro and in vivo test methods used during preclinical development. In most cases, human gastrointestinal physiology is not properly considered, which leads to the application of inappropriate in vitro and animal models. Moreover, conditions in the stomach are often not fully understood. Important aspects such as the kinetics of fluid volumes, gastric pH or mechanical stresses have to be considered in a realistic manner, otherwise, the gastroretentive potential as well as drug release of novel formulations cannot be assessed correctly in preclinical studies. This review, therefore, highlights the most important aspects of human gastrointestinal physiology and discusses their potential implications for the evaluation of gastroretentive drug delivery systems. Full article
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Open AccessReview
Current State and Future Perspectives on Gastroretentive Drug Delivery Systems
Pharmaceutics 2019, 11(4), 193; https://doi.org/10.3390/pharmaceutics11040193 - 20 Apr 2019
Cited by 2
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 [...] Read more.
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. Full article
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