Gastroretentive Drug Delivery System Research Articles

A recent update on gastro retentive drug delivery systems

Gastro retentive drug delivery systems (GRDDS) have garnered significant attention in recent years due to their potential to enhance therapeutic efficacy and patient compliance by prolonging gastric residence time and optimizing drug release kinetics. This review provides a comprehensive overview of the latest advancements in GRDDS, focusing on formulation strategies, design principles, and evaluation methodologies. Various approaches such as floating systems, mucoadhesive systems, expandable systems, and magnetic systems are discussed in detail, highlighting their mechanisms of action and applications in targeted drug delivery. Furthermore, recent innovations in materials science and formulation technologies have enabled the development of novel GRDDS with improved biocompatibility, stability, and controlled release profiles. The review also addresses challenges associated with GRDDS, including physiological variability, drug stability, and regulatory considerations, and proposes potential strategies to overcome these obstacles. Additionally, the clinical relevance of GRDDS in the treatment of various gastrointestinal disorders and their future prospects in personalized medicine and targeted therapy are explored. Overall, this review aims to provide valuable insights into the current state-of-the-art in GRDDS research and its implications for the advancement of drug delivery science.

New Trends in Emerging Novel Nanosponges Drug Delivery

Medical professionals have long had trouble delivering medications to the correct location in the body and controlling their release to prevent overdose. Nano-sponges are novel and complicated molecules, which have the ability to alleviate these challenges. Utilizing nano-sponges allows for precise drug delivery to the desired location. Nano-sponge technology gets better patient compliance by delivering drugs to strategic locations while also extending dosing intervals. Various drug delivery techniques, such as parenteral, transdermal, oral, and immunosuppressive drugs, involve Nano-sponges. In today's world, nanosponges are used in gastro-retentive drug delivery systems.

Design and Characterization of Hallow Porous Floating Microspheres of Favipiravir

The present investigation deals with the design and characterization of favipiravir floating microspheres for gastro retentive drug delivery system by employing 3² factorial design and also to investigate the main effects of different independent variables on microspheres that float. The emulsion solvent diffusion method was used to manufacture floating microspheres with Eudragit S 100 as the polymer. These microspheres will extend the release of the medicine, reducing the frequency of administration and the harmful effects caused by fluctuations in plasma concentration with conventional dosage forms. The main effect of independent variables like polymer Eudragit S 100 concentrations (50, 100, 150 mg) and stirring time (1, 2 and 3 hours) on the performance of microspheres. Formulated microspheres were characterized for responses including drug release, particle size, and entrapment efficiency and floating time. Based on the results of the responses, the optimized composition was arrived using the response surface method graphical and numerical optimization method using design of experiments (DoE) software. Then, the optimized formulation (OFES) was prepared and evaluated for the four responses compared with predicted values to find the validity of the selected model. The optimized formulation was further analyzed for drug-excipient compatibility by fourier-transform infrared (FTIR), differential scanning calorimetry (DSC), and also analyzed by X-ray diffraction (XRD), scanning electron microscope (SEM) analysis. Further zeta potential and micrometric properties were also observed. The results for the formulation FES 1 to 9 found were, that particles size ranged from 0.192 to 0.277 μm, entrapment efficiency ranged from 68.65 ± 1.9 to 76.25 ± 3.2%, percentage drug release range was from 89.25 ± 0.24 to 93.68 ± 0 .25%, and floating time range was from 12 to 23 hours. As per the design, OFES an optimized formulation fitted with the concentration of Eudragit S 100 of 139.1 mg and stirring time of 1-hour. Regarding the kinetic release, the responses were best fitted with Higuchi model of R² value of 0.9795 with kinetic mechanism of non-fickian diffusion with R² value of 0.9499, indicating good linearity. The combination of different variables and their effects on responses were investigated well using factorial design, and an optimized formulation was developed for favipiravir.

A Review on Gastro-Retentive Drug Delivery System

The aim of this review is to focus on the various gastro retentive approaches by investigate, compile, and present in most concise way, where the gastroprotective has gained immense popularity in the field of oral drug delivery. In the field of oral drug delivery gastro-retentive drug delivery play an important role. There are various types of GRDDS approaches which can be utilized to retain the dosage form in the stomach and release the drug slowly for an extended period of time. The various GRDDS approaches include high density, low density, mucoadhesive, expandable, magnetic systems and super porous hydrogel system. GRDDS has proved to be effective in both local and systemic actions to treat gastric or duodenal ulcers. Gastro-retentive drug delivery system can be utilized to prolong the residence time of delivery system in the stomach. Where the stomach and duodenum are separated by the pylorus, which has an important role in residence time of the ingested substances in the stomach. GRDDS can be used to overcome challenges related with conventional oral dosage forms. Keywords Gastro-retentive, GRDDS, Oral route, GIT, various approaches, floating system, non-floating system, bio adhesive system.

Gastroretentive Drug Delivery Systems with improved Floating and Swelling Capabilities

For medications with an absorption window in the stomach and upper part of small intestine, a controlled drug delivery system with a longer stomach residence duration can be particularly useful. Rapid gastrointestinal transit may cause drug delivery system above the absorption zone to only partially release drug, which would reduce the supplied dose's effectiveness. The main drawbacks are linked to the non-uniformity of drug absorption across the alimentary canal and the inter- and intra-subject variability of gastro-intestinal transit time. The bioavailability of medications is predicted to be improved by floating delivery systems, which are designed to stay buoyant on the gastric contents for an extended period of time. Floating in combination with swellable system gaining attention due to their wide applicability in the targeting of drugs to stomach. These floating and swellable tablet have the advantage that they remain buoyant and swells to 2-3 folds in gastric fluid.

Recent Advances in Gastro Retentive Drug Delivery Systems

The issues with oral conventional dose forms can be resolved with the use of gastroretentive drug delivery systems (GRDDS). GRDDS is a way to prolong the stomach residence time, which allows for the release of drugs and the possibility of local or systemic effects in the upper gastrointestinal tract. To enhance treatment, some potent medications are employed with gastro-retentive dose forms for longer. By producing a high concentration of medication in the stomach that can be sustained for an extended amount of time, gastroretentive formulations (GRFs) greatly improve stomach pharmacotherapy. As a result, a wide range of dosage forms have been developed for medications that break down at alkaline pH but remain stable at acidic pH. Therefore, medications have limited absorption.

A Comprehensive Review on Floating Drug Delivery System

The category of gastroretentive drug delivery systems (GRDDS) includes floating drug delivery systems (FDDS). These dose formulations are intended to extend the duration of the stomach's residence period by a sustained release technique. Drugs which are harder to dissolve in high pH environments have improved bioavailability and solubility when incorporated into GRDDS. Reduced intestinal absorption of solid dose forms can be accomplished by the flotation mechanism. The novel fusion of bilayer and floating mechanism is demonstrated by the bilayer floating drug delivery device. It demonstrates the effective creation of a controlled release formulation. Bilayer floating tablets offer a sustained release layer formulation in addition to an immediate release. A attempt was made to explain the mechanism of FDDS, or floating bilayer, in the review. In order to accomplish regulated administration of various medications with predetermined release profiles, bi-layer tablets were developed. The pharmaceutical industry has been more interested in creating bilayer tablets over the past ten years as a way to improve patient compliance and convenience by combining two or more API in a single dose form.

Gastroretentive drug delivery system: An Overview

Gastric emptying is a complex and incredibly factor process. This causes the unusualness of the bioavailability of medication delivery system. GRDDSs can improve the controlled delivery of medications that have an ingestion window by continuously delivering the medication for a delayed time before it arrives at its assimilation site. Gastro retentive drug delivery system (GRDDS)s have gotten huge consideration in the previous many years, because of the way that they can overcome the limitations of regular oral controlled released drug delivery system identified with quick gastric emptying time. An ideal GRDDS can be characterized as a system which stays in the stomach for an adequate time and deliver the active ingredients in a controlled way so that sustained action can be created. This, altogether broadens the duration of medication release, prolongs dosing interval and expands bioavailability of medications and consequently improves compliance of the patients and viability of pharmacotherapy. This article gives an outline of the fundamental ideas used to design drug dosage form with delayed gastric residence time as well as the factors influencing gastric emptying, favourable circumstances, deficiencies, formulation consideration and, elements that influence gastro retentive system. The principal emphasis is on the whole grouping and various types of GRDDSs.

New Carriers for Bioadhesive Gastroretentive Drug Delivery Systems Based on Eudragit® EPO/Eudragit® L100 Interpolyelectrolyte Complexes

The aim of this study was the analysis of interpolyelectrolyte complexes (IPECs) based on Eudragit® EPO and Eudragit® L100 as prospective carriers for gastroretentive drug delivery systems (GRDDS) using two model drugs: metronidazole (MZ) and acyclovir (ACR). Eudragit® EPO/L100 IPECs with different pH concentrations were characterized by different degrees of swelling in mimicking fasted stomach medium (0.1 M HCl) and saved their shape for 6 h. The microenvironmental changes in IPEC structures in acidic medium were investigated using FT-IR spectroscopy, thermal and elemental analysis. IPEC samples showed bioadhesive properties that were not significantly different from the positive control (Carbopol) in the test with the mucin compacts. The release rate of metronidazole (class I BCS) from IPEC matrices increased with the increasing degree of swelling. IPEC 1 provided 49.62 ± 6.20% and IPEC 2 reached 87.69 ± 5.15% of metronidazole release after 6 h in mimicking fasted stomach medium (0.1 M HCl). The total amount of released acyclovir (class III BCS) from IPEC 1 was 25.76 ± 5.67% and from IPEC 2 was 21.48 ± 5.00%. Release of both drugs was controlled by relaxation of polymeric chains in matrices according to the Peppas–Sahlin model. According to the received results, investigated interpolymer complexes are prospects for further evaluation as carriers for gastroretentive bioadhesive systems.

Gastro Retentive Drug Delivery System: Latest Approach towards Novel Drug Delivery

Various efforts have been undertaken to enhance the bioavailability and clinical performance of oral drug formulations. In pursuit of improving the therapeutic effectiveness of medications that are susceptible to degradation in alkaline pH environments, possess a limited window for absorption within the stomach, and readily dissolve under acidic conditions, a diverse range of gastro-retentive drug delivery systems (GRDDS) have been innovatively designed and developed. As a result, the stomach’s physiological state and the various factors that influence GRDDS will be discussed. As a rule, this survey will enlighten and coordinate enumerating scientists in arranging, plan, and planning the GRDDS.

Preparation and evaluation of luteolin-loaded PLA-based shape memory gastroretentive drug delivery systems

Luteolin, a natural flavonoid, is gaining growing attention for its potential in the treatment of gastric cancer. However, its clinical application is limited by factors such as poor aqueous solubility. This study aimed to develop a novel gastroretentive drug delivery system (GRDDS) to both enhance the oral bioavailability of luteolin and prolong its release and in vivo circulation time. Out of 10 luteolin-loaded PLA-based shape memory films prepared in this study, the LPC-PLA/PEG(7/3) formulation incorporated with PEG, HPMC, and NaHCO3 exhibited optimal properties in terms of drug release and inhibitory activity against SGC-7901 cells. Moreover, small-animal imaging revealed that LPC-PLA/PEG(7/3) exhibited a prolonged gastric retention time of approximately 8 h. Furthermore, the pharmacokinetic studies indicated a 354 % increase in the oral bioavailability of LPC-PLA/PEG(7/3) in rats compared to luteolin. In sum, a novel GRDDS was developed to enhance the relative bioavailability of luteolin, offering a potential strategy for practical oral administration.

Gastro Retentive ( Floating) Delivery System

Because of its flexibility in formulation, ease of administration, and patient compliance, the oral route of drug administration is the most preferred route. However, this route has some limitations, such as a limited gastric residence time (GRT) for sustained drug delivery systems and drugs that are absorbed from a specific region of the gastrointestinal tract (GIT). To overcome these limitations, various approaches to increasing the gastric retention time of the delivery system in the upper gastrointestinal tract have been proposed. The gastroretentive dosage form (GRDF) extends the GRT by directing drug release to the upper part of the GIT. GRDFs enable continuous and prolonged drug release and improve bioavailability of drugs with a narrow therapeutic window, thereby extending dosing intervals and increasing patient compliance. This article's goal is to compile the various gastroretentive approaches. We have summarized important factors controlling gastric retention in order to understand the various physiological difficulties in achieving gastric retention. Finally, the parameters for evaluating gastroretentive drug delivery systems are discussed. The current review briefly discusses the current state of various leading Until now, gastroretentive drug delivery technologies such as high density (sinking), floating, bio- or mucoadhesive, expandable, unfoldable, super porous hydrogel, magnetic systems, and so on have been developed. Furthermore, important factors controlling gastroretention, benefits, and future potential are discussed.

Formulation and Characterization of Gastroretentive Drug Delivery System of Teneligliptin

The aim of the study is an attempt to prepare and characterize the Teneligliptin floating tablets. Drugs having a short half life are eliminated quickly from the blood circulation. Several controlled delivery systems have been designed which can overcome the problems of unpredictable gastric emptying due to physiological problems and presence of food and also release the drug to maintain its plasma concentration for a longer period of time. The Teneligliptin a orally administered of BCS class-2 drug, which has low solubility and high permeability, which is widely use in the management of type 2 diabetes, is an oral anti- hyperglycemic agent, shows incomplete absorption from the gastrointestinal tract and from the gastrointestinal track and absolute bioavailability is 40-70%. This has to development of oral gastro retentive floating dosage forms.Teneligliptin is a DPP4 inhibitor and is to exert its mechanism of action on management of Type 2 Diabetes mellitus. Teneligliptin is poorly soluble in acidic environment and hence the absorption of drug to diabetic patient is slow due to this gastric motility and emptying capacity.Thus it can be converted into a suitable dosage form like Floating Drug Delivery System. Around 10 formulations were prepared and are characterized by various pre compression and post compression evaluation studies. The preformulation results of Angle of repose, Bulkdensity, Tapped density, Compressibility index, and Hausner’s ratio were found to be within pharmacopoeial limit.The post compression evaluation results of all formulation were within the pharmacopeial limit. The present study revealed that the Teneligliptin can be formulated to enhance the bioavailability which can reduce the frequency of dose.

Gastro Retentive Drug Delivery System: A Review

Gastro Retentive Drug Delivery Systems (GRDDs) are an approach to prolonging gastric residence time by targeting the release of specific drugs at the top of the GIT for local or systemic effect. The Gastro Retentive Dosage Forms (GRDFs) is a very long-term time used to improve treatment with several important drugs. GRDDs are one example of a novel strategy to extending gastric residence duration, concentrating on the local or systemic effects of particular medications released in the stomach. GRDFs can provide prolonged and continuous drug release to the upper part of the Gastro Intestinal System (GIT), which greatly extends the duration of the drug release, improves the bioavailability of drugs with narrow therapeutic windows, and thus extends the dose interval and improves the patient's compliance. GRDFs enable the drug to be released longer and continuously to the upper part of GIT, thereby significantly extending the time when the drug is released and improving the bioavailability of a drug with narrow therapeutic windows, thus prolonging the dose interval and increasing patient compliance.

Developing and scaling up captopril-loaded electrospun ethyl cellulose fibers for sustained-release floating drug delivery

In this work ethyl cellulose (EC) was used as a matrix polymer and loaded with captopril, with the goal to fabricate electrospun fibers as potential sustained-release floating gastro-retentive drug delivery systems. Fibers were prepared with monoaxial and coaxial electrospinning, and both bench-top and scaled-up (needle-based) methods were explored. With monoaxial electrospinning, EC-based fibers in the shape of cylinders and with smooth surfaces were obtained both at 1 and 20 mL/h. For coaxial electrospinning, the drug was encapsulated in the core and fibers generated with core/shell feeding rates of 0.5/1 and 5/10 mL/h. These fibers were cylindrical in shape with a wrinkled surface, and confocal microscopy suggested them to have a core/shell structure. X-ray diffraction and differential scanning calorimetry results showed that all the fibers were amorphous. The encapsulation efficiency of all the formulations was almost 100%. Release studies in simulated gastric fluid indicated that the monoaxial electrospun fibers gave slower release profiles compared with a physical mixture of captopril and EC, but there was still an initial “burst” of release at the start of the experiment. Fibers with low drug-loading (9.09% w/w) showed a slower release than fibers with high loading (23.08% w/w). The coaxial fibers exhibited sustained release profiles with reduced initial burst release. Both monoaxial and coaxial fibers could float on the surface of simulated gastric fluid for over 24 h at 37 °C. After storage under ambient conditions (19–21 °C, relative humidity 30–40%) for 8 weeks, all the fibers remained amorphous and the release profiles had no significant changes compared with fresh fibers. This work thus highlights the potential of coaxial electrospinning for fabricating a sustained-release floating gastro-retentive drug delivery system for captopril.

Facts and Features of Gastroretentive Drug Delivery System

Oral drug delivery has gained a lot of popularity because of patient compliance and the simplicity of administration. It only provides a small number of benefits for medications with poor bioavailability because of inadequate digestion and absorption in the latter stages of the GI tract. In this scenario, GRDDS have emerged as a preferred choice for drug administration with unique qualities such as a narrow absorption window, avoiding metabolism, instability in high alkaline pH, and improved solubility in low pH. In this present review, we discuss the Merits and demerits, the physiology of the stomach, and factors affecting the grdds. Various gastrointestinal technologies, including floating, non-floating, expandable, superporous hydrogel; Bioadhesive, magnetic, and raft system, as well as their applications, is outlined. In addition, potential future developments on this technology to minimise stomach emptying rate in both fasting and fed stages are highlighted. In the end, this review might assist formulation scientists and researchers in designing the GRDDS.

Sodium alginate-based smart gastro-retentive drug delivery system of revaprazan loaded SLNs; Formulation and characterization

Revaprazan (REV), a novel reversible Proton Pump Inhibitor (PPI) used to treat peptic ulcers, faces challenges in therapeutic efficacy due to its poor dissolution properties and a short half-life. Solid lipid nanoparticles (SLNs) have emerged as a drug delivery system capable of enhancing dissolution and bioavailability of lipid soluble drugs. Here, we report on the development and optimization of a smart gastro-retentive raft system of REV-loaded SLNs (GRS/REV-SLNs) to enhance drug bioavailability and gastric retention. The optimized REV-SLNs had a particle size of 120 nm, a Polydispersity Index (PDI) of 0.313, a zeta potential of −20.7 mV, and efficient drug incorporation of 88 %. Transmission Electron Microscopy (TEM) affirmed the spherical morphology of these REV-SLNs, while Fourier Transform Infrared Spectroscopy (FTIR) revealed no chemical interactions among components. In-vitro assessment of the final GRS/REV-SLNs demonstrated sustained gelation and buoyancy for over 12 h, which would significantly enhance REV retention and its release within the stomach. Further assessments in rats confirmed successful gel transformation within the stomach, resulting in the improved bioavailability of REV. Thus, the development of GRS/REV-SLNs significantly improved the delivery and bioavailability of REV within the stomach, and offers a potentially improved method of treating peptic ulcers.

Effect of using high molecular weight crosslinker on the physical properties of super porous hydrogel composite

Superporous hydrogel composite is widely utilized and investigated as a gastro retentive drug delivery system. Materials used in Superporous hydrogel formulation have a profound effect on its properties’, N-methylene bisacrylamide is the crosslinker of choice for the preparation of SPH.
 The purpose of this study is to determine if using a new high molecular weight crosslinker such as polyethylene glycol diacrylate will affect the physical characteristics of SPH and drug release behavior. For the preparation of super porous hydrogel polyvinyl alcohol, acrylamide, polyethylene glycol diacrylate 700, N, N-Methylene bisacrylamide, sodium bicarbonate, and tween 20 were used. Trifluoperazine HCl was used as a model drug. The buoyancy, porosity, density, drug release, drug content, swelling ratio, and swelling time were studied and compared. All the physical characteristics and medication release profiles were impacted by changing the formulation parameters. The formula with the best physical qualities had 300 µl of acrylamide (40 percent w/v), 20 mg of polyvinyl alcohol, 200 µl of Tween 20 (v/v), 5 µl of polyethylene glycol diacrylate 700, 45 µl ammonium persulfate, 45 µl TEMED and 50 mg of sodium bicarbonate. Around 80% of the drug was released over the course of 12 hours according to zero order kinetics. By modifying the formulation parameters using polyethylene glycol diacrylate, Superporous hydrogel was successfully manufactured and has the best properties to be employed as a gastro retentive drug delivery system.

Development and Characterization of Febuxostat Loaded Floating Beads as Gastro-retentive Drug Delivery System in the Treatment of Gout: A Statistical Approach

Background: Febuxostat is a BCS class-II drug, used in the treatment of gout. However, because of its lower solubility, a higher and more frequent dose of the drug is required in the treatment. Objective: The objective of this research was to develop and evaluate febuxostat-loaded floating beads as a gastro-retentive drug delivery system (GRDDS) to target drug release up to 24hr in order to enhance bioavailability. Methodology: Gastro-retentive floating beads were formulated using the ionotropic gelation method. Screening of lipids was carried out based on the shape and texture of floating beads. Drug-excipient compatibility study was done using DSC analysis. Further optimization of gastro-retentive floating beads of febuxostat was performed by Box-Behnken design using gelucire 43/01, lactose, and soluplus as independent variables and %drug entrapment and %drug release after 24 hr as dependent variables. Evaluation of the optimized batch was performed for in vitro buoyancy, %drug entrapment, %drug release, FTIR, and SEM study. Result and Discussion: In the ANOVA, contour plots, and 3D surface plots, the optimized batch showed 93.95±0.29 % drug entrapment and 88.14±0.58 % drug release after 24 hr with 98%±1% invitro buoyancy. Overlay plots and checkpoint batches were accompanied to confirm the optimization. Polynomial equations proved the positive effect of lipids on drug entrapment and drug release. SEM images explained porous and microstructures on beads. Conclusion: In conclusion, gastro-retentive febuxostat floating beads were successfully developed and characterized for once a daily dose with enhanced bioavailability and reduced cost of therapy.

In Situ Gelling Gastro-retentive Raft Containing Ficus racemosa Fruit Extract: A Promising Approach to Treat GERD

Gastro-retentive drug delivery system has been widely used to prolong retention of dosage forms in stomach. Amongst various formulations and approaches, the raft formulations sustain the drug release as well as prolonged gastric retention, along with the added advantage of liquid dosage forms. The present study was an attempt to formulate and evaluate Raft forming floating gel for the extract of Ficus racemosa unripe fruit also known as Udumbar or Audumbar which is recognized for the treatment of ulcerative diseases in Ayurveda. To prepare the raft formulation natural polymers such as Gellan Gum, Xanthan Gum and Guar Gum were used along with gas forming ingredients. The formulations were prepared using 32 factorial design. The raft formulations are expected to prolong the retention of the medicinally active extract in stomach for longer duration of action. The evaluation was carried out for floating behavior, gel strength, viscosity, and in vitro dissolution for the gastro-retentive gels. The formulations were found to have floating duration upto 05 hr with a sustained release of active medicament.