Development of Gabapentin Expandable Gastroretentive Controlled Drug Delivery System

Abstract

Expandable drug delivery systems are one of many gastroretentive delivery systems which have emerged during the last few years. Expandable systems are usually folded in a capsule and expand to dimensions greater than the pyloric sphincter upon contact with gastric fluid. This prevents them from being evacuated by gastric emptying. The main objective of developing such systems is to increase the residence time of a specific drug in stomach; controlling its release, increasing its bioavailability and decreasing its side effects and dosing frequency. An expandable gastroretentive drug delivery system containing Gabapentin was developed using experimental design (D-optimal reduced quadratic design). This system was able to unfold at stomach pH in less than 15 minutes and obtain a controlled release of 78.1 ± 4.7% in 6 hours following zero-order release kinetic model. It is rigid in stomach and its rigidity decreases at intestinal pH. FTIR analysis indicated the occurrence of hydrogen bonding in Gabapentin when present in the developed system, which might be responsible for the drug’s controlled release. XRD analysis indicated that Gabapentin physical properties changed from crystalline in the typical state to amorphous in the developed system.

Gastroretentive Technologies in Tandem with Controlled-Release Strategies: A Potent Answer to Oral Drug Bioavailability and Patient Compliance Implications

“…When activated, it generated carbon dioxide gas that helped push the folded parts away from each other. Furthermore, the release of gabapentin was retarded for longer than 6 h and followed zero-order kinetics [161].…”

“…When activated, it generated carbon dioxide gas that helped push the folded parts away from each other. Furthermore, the release of gabapentin was retarded for longer than 6 h and followed zero-order kinetics [161]. Xanthan gum has shown promising properties as a swelling and expanding agent either used solely or in combination with other materials, such as guar gum [162].…”

“…Rimawi et al developed an expandable matrix system in the form of a layer that contained gabapentin as the API. Gelatin was used as a swellable hydrophilic polymer which increased in size upon contact with the body fluids, as well as a plasticizer (Poloxamer 407) that increased the flexibility of the layer, and hydrophobic polymers (Eudragit ® L100, L100-55 and S100) as release retarding agents [161]. The system was able to unfold and expand within 15 min to a diameter larger than 20 mm after contact with hydrochloric acid dissolution medium which could potentially prevent a premature evacuation of the system from the stomach (Figure 7).…”

Administration strategies and smart devices for drug release in specific sites of the upper GI tract

“…Various scientists worked independently on expandable GR DDSs in a similar film-like structure [41,[91][92][93][94][95][96][97][98]. This largely represented the most investigated geometry at the research level, probably for its design simplicity.…”

Floating Microspheres of Lafutidine: Formulation, Optimization, Characterization, in-vitro and in-vivo Floatability Studies Using Eudragit Grades

“…Gastroretentive delivery systems are mainly intended for drugs having a narrow absorption window, a biological half-life ranging from 2-8 hr and drugs taken in multiple daily doses. 5 The GRDDS greatly improves the pharmacotherapy of the stomach through local drug release, leading to high drug concentrations at the gastric mucosa. 6 Micro particulate drug delivery system has recently attracted a lot of attention of scientists working in the area of drug delivery as in addition to other advantages associated with gastro-retentive drug delivery, they also avoid all or none effects associated with unit dosage forms thereby ensuring the success of therapy.…”