Industrial perspective of gastroretentive drug delivery systems: Physicochemical, biopharmaceutical, technological and regulatory consideration

Abstract

Pharmacotherapy of various disease states can be amended by drug repurposing through GRDDS. Assessment of the effect of the fed and fasted condition on product performance should be necessary during initial development phases. Dual working technology would be a possible way to overcome drawbacks associated with different GRDDS. Before development of a drug product, the principles of scale up and process validation must be considered to improve the quality and market availability of GRDDS. Knowledge of all regulatory aspects will help to deliver a product to the market within a reasonable timeframe and in a cost-effective manner.

Fused Deposition Modeling (FDM) 3D Printed Tablets for Intragastric Floating Delivery of Domperidone

“…A short gastric residence time may result in incomplete drug release from the delivery vehicle, subsequently leading to poor therapeutic effect 2 . Several novel gastroretentive delivery systems have been explored to overcome the shortcomings above, including polymer bioadhesive systems, swelling and expanding systems, high-density systems and floating systems 3 . The floating systems are low-density systems that have sufficient buoyancy to float over the gastric contents and remain in the stomach for a prolonged and predictable period 4 .…”

Decades of research in drug targeting using gastroretentive drug delivery systems for antihypertensive therapy

“…GRDDS can be a viable option for management of hypertension management as several antihypertensive drugs are associated with (a) narrow absorption window {e.g. furosemide (Pawar et al, 2012;Davis, 2005;Darandale, Vavia, 2012), atenolol, diltiazem (Srikanth et al, 2011)}; (b) short half-life {e.g. losartan (Chen et al, 2010), furosemide (Darandale, Vavia, 2012)}, (c) instability {e.g.…”

“…losartan (Chen et al, 2010), furosemide (Darandale, Vavia, 2012)}, (c) instability {e.g. captopril (Streubel, Siepmann, Bodmeier, 2006;Pawar et al, 2012)} at high pH values; (d) low solubility {e.g. verapamil (Streubel, Siepmann, Bodmeier, 2006;Niranjanbhai et al, 2012), furosemide (Streubel, Siepmann, Bodmeier, 2006), propranolol (Chinta et al, 2009)} at high pH, and (e) degradation in the colon {e.g.…”

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“…Floating or bioadhesive approaches have some merits and demerits it can be reduced by the combination of these two different approaches. [13] Floating system means that float over the surface of the gastric contents when the stomach is full after a meal but at the time stomach as empties and the tablet reaches the pylorus the buoyancy of the dosage may be decreased as dosage forms passages through the pylorus and it highly dependent on the presence of food and gastric content. In bioadhesive system, it is quite likely that they become dislodged from the stomach wall when the system is full, and the semi-liquid contents are churning around due to the effect of peristalsis and its efficiency can be reduced by the constant turnover of the mucus.…”

“…[10] Low-density excipients and polymers are used for manufacturing of FDDS. [11,12] These GRDDS approaches have some merits and demerits like FDDS is effective only when the fluid level in the stomach is sufficiently high [13] as the stomach empties and the tablet is at the pylorus, the buoyancy of the dosage form may be impeded. Bioadhesive system it is quite likely that they become dislodged from the stomach wall when the system is full, and the semi-liquid contents are churning around due to the effect of peristalsis and its efficiency can be reduced by the constant turnover of the mucus.…”