Superporous Hydrogels Research Articles

Gastroretentive Swellable and Floating Systems: An Innovative and Promising Strategy for Drug Delivery-A Comprehensive Review

Gastroretentive drug delivery systems (GRDDs) have emerged as an innovative and promising approach for enhancing the bioavailability and therapeutic efficacy of drugs with narrow absorption windows in the upper gastrointestinal tract (GIT). Among various GRDDs, swellable and floating systems have garnered significant attention due to their ability to prolong gastric residence time, improve drug dissolution, and facilitate sustained drug release (SDR). This comprehensive review provides a detailed exploration of the principles, mechanisms, and advancements in swellable and floating Gastroretentive systems. The key strategies, such as the use of hydrophilic polymers, gas-generating agents, and superporous hydrogels, are discussed. These systems offer benefits in treating conditions like peptic ulcers, gastroesophageal reflux disease, and infections, where prolonged localized drug action is desirable. A critical assessment of recent preclinical and clinical studies highlights the therapeutic potential of GRDDs in optimizing drug delivery for poorly soluble drugs and drugs with short half-lives. Challenges such as variability in gastric retention, potential toxicity of excipients, and patient-specific factors are also examined. It includes the outlining future trends in GRDDs, focusing on the incorporation of nanotechnology, 3D printing, and biocompatible materials to overcome existing limitations and further enhance therapeutic outcomes. This highlight of review article is initially introduction of GRDDs and their significance, mechanism and their classification of GRDDs, intermediately describe brief on swelling and floating GRDDs system with their application, lastly it describes the recent advances in patent, clinical trials and marketed products for GRDDs swellable and floating system. Keywords: Drug delivery; GRDDs; floating; swellable; gastroretentive; system; advance approach

Design, fabrication, and in-vitro characterization of pHresponsive sustained-release super porous hydrogel containing metformin HCl

Design, fabrication, and in-vitro characterization of pHresponsive sustained-release super porous hydrogel containing metformin HCl

Superporous Hydrogels as Super Disintegrants in Formulating Oral Disintegrating Tablets of Clozapine for the Treatment of Schizophrenia.

In this study, clozapine was formulated as orally disintegrating tablets (ODTs) using a direct compression method, incorporating super porous hydrogels as superdisintegrants. The disintegration time, hardness, friability, and stability of these ODT formulations were systematically evaluated, along with detailed dissolution profiles. Surprisingly, friability measurements revealed values below 1%. All tablet formulations disintegrated completely within 1 minute, meeting the 3-minute disintegration time criterion specified by the USP for ODTs. Moreover, over 85% of the labeled clozapine content was dissolved within 15 minutes from the ODTs. FTIR analysis indicated no interaction or alterations between the active ingredient and excipients. Consequently, the ODT formulations prepared using super porous hydrogels as superdisintegrants represent a promising strategy. This approach could significantly aid in the development and manufacturing of generic clozapine products.

Preparation and in vitro characterization of graphene oxide impregnated superporous hydrogel beads: an effective approach of gastro-retentive drug delivery system

ABSTRACT The remarkable properties of graphene oxide, a shining dynamo, opened new possibilities for delivering the drug. The present work aims to fabricate a graphene-based porous hydrogel system that fades its side effects and encourages its utilization as a drug carrier. Graphene oxide was impregnated in the polymeric matrix for gastro-retentive drug delivery. Porogen was added to create a superporous structure. The extrusion-dripping technique is used to fabricate low density, super porous, and floating hydrogel beads, which were considered a practical approach to target the drug in a controlled and sustained manner in the stomach. The fabricated graphene oxide impregnates superporous beads were characterized by physicochemical analysis, morphological parameters, PXRD, swelling study, drug-release pattern, and in-vitro floating ability. The homogenous nature of fabricated samples was analyzed by weight and size variation. Micrometric properties were estimated to calculate the density and flow ability of superporous beads. The stability and shelf life of prepared hydrogels were performed by accelerated stability analysis according to ICH guidelines. Doxorubicin was chosen as a model anticancer drug. The pi–pi stacking technique is responsible for a considerable loading of the drug onto graphene oxide (GO). However, the successful preparation of low-density graphene oxide impregnates superporous hydrogel beads shows excellent floating ability, thus making it a promising candidate for stomach targeting.

Development of high efficacy super-porous hydrogel composites-based polymer desiccants to capture water vapors from moist air

Development of high efficacy super-porous hydrogel composites-based polymer desiccants to capture water vapors from moist air

Superporous Hydrogel: A Novel Approach for Safe Gastroretentive Drug Delivery System

Superporous hydrogel are developed initially as novel drug delivery system to retain dosage form in upper gastrointestinal tract, and absorbs drug in gastric medium. The generation-based classification of superporous hydrogel is covered in this review. The hydrophilic polymer networks formed by the molecular entanglements which absorb water up to thousands of times to their dry weight. These systems swells quickly and resist in an extremely acidic condition in stomach. This hydrogel is instantly swell through capillary force which is driven by absorption of water through an open porous structure. This system provides better solubility and bioavailability by targeting the specific site of absorption. The conventional superporous hydrogels have the poor mechanical strength which is overcome by developing the second superporous hydrogel generation composites and the third-generation superporous hydrogel hybrids. This article has mainly focused on the classification, techniques, drug loading, research papers, characterizations and applications of superporous hydrogel.
 Keywords: Gastric retention, Cross-linking, Superporous hydrogel, Swelling rate, Elastic property, Hydrophilic polymer networks.

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.

Fabrication and evaluation of Dillenia indica-carrageenan blend hybrid superporous hydrogel reinforced with green synthesized MgO nanoparticles as an effective wound dressing material

An unexplored hybrid superporous hydrogel (MHSPH) of Dillenia indica fruit mucilage (DIFM) and carrageenan blend embedded with green synthesized magnesium oxide nanoparticles (MNPs) is utilized as an effective wound dressing material with appreciable mechanical strength in murine model. The prepared MNPs and the optimized MHSPH were characterized using X-ray diffraction (XRD), thermogravimetric analysis (TGA), Fourier transform infrared (FT- IR) spectroscopy. Size, zeta potential and morphology of MNPs was assessed using Dynamic light scattering technique (DLS) and field-emission scanning electron microscopy (FESEM) respectively. The MHSPH grades were further optimized using swelling study in phosphate buffer solution at pH 1.2, 7.0, and 8. Both MNPs and the optimized grade of MHSPH were evaluated based on hemolysis assay, and protein denaturation assays indicating them to be safe for biological use. Acute toxicity studies of the optimized MHSPH on Zebra fish model, revealed no observable toxic effect on the gill cells. Wound healing in Swiss albino mice with application of optimized grade of MHSPH took only 11 days for healing when compared to control mice where healing took 14 days, thus concluding that MHSPH as an effective dressing material as well as tissue regrowth scaffold.

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.

Evaluation of Opuntia-carrageenan superporous hydrogel (OPM-CRG SPH) as an effective biomaterial for drug release and tissue scaffold

The process of wound healing involves complex interplay of systems biology, dependent on coordination of various cell types, both intra and extracellular mechanisms, proteins, and signaling pathways. To enhance these interactions, drugs must be administered precisely and continuously, effectively regulating the intricate mechanisms involved in the body's response to injury. Controlled drug delivery systems (DDS) play a pivotal role in achieving this objective. A proficient DDS shields the wound from mechanical, oxidative, and enzymatic stress, against bacterial contamination ensuring an adequate oxygen supply while optimizing the localized and sustained delivery of drugs to target tissue. A pH-sensitive SPH was designed by blending two natural polysaccharides, Opuntia mucilage and carrageenan, using microwave irradiation and optimized according to swelling index at pH 1.2, 7.0, and 8.0 and % porosity. Optimized grade was analyzed for surface hydrophilicity-hydrophobicity using OCA. Analytical characterizations were performed using FTIR, TGA, XRD, DSC, reflecting semicrystalline behavior. Mechanical property confirmed adequate strength. In vitro drug release study with ciprofloxacin-HCL as model drug showed 97.8 % release within 10 h, fitting to the Korsmeyer-Peppas model following diffusion and erosion mechanism. In vitro antimicrobial, anti-inflammatory assays, zebrafish toxicity, and animal studies in mice with SPH concluded it as a novel biomaterial.

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.

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.

Green synthesis of quince/pectin cross-linked superporous hydrogel sponges for pH-regulated sustained domperidone delivery

The present study aims to utilize green synthesis to fabricate stimuli-responsive, smart, quince/pectin cross-linked hydrogel sponges for the pH-regulated conveyance of domperidone. The designed hydrogel sponges were evaluated for a sol–gel fraction (%), swelling studies and kinetics, drug loading (%), electrolyte-responsive character, scanning electron microscopy (SEM), thermal analysis, drug-excipient compatibility studies (FTIR), X-ray diffraction (XRD) analysis, mechanical testing, in-vitro drug release studies, and acute oral toxicity studies. The drug loading (%) ranged from 67 to 85%. Hydrogel sponges displayed pH-responsive swelling potential, with optimum swelling in a phosphate buffer (pH 7.4) and insignificant swelling in an acidic buffer of pH 1.2. The prepared hydrogel sponges displayed second-order swelling dynamics. The FTIR data revealed the successful fabrication of the hydrogel sponges with the primary drug peaks remaining unchanged, demonstrating excipients-drug compatibility. SEM confirmed the rough, porous surface of hydrogel sponges with numerous cracks. XRD measurements revealed the transformation of the crystalline nature of domperidone into an amorphous one within the developed hydrogel sponges. Dissolution studies revealed little domperidone release in an acidic environment. However, hydrogel sponges exhibited release up to 10 h in phosphate buffer.The sponge's non-toxic or biocompatible character was confirmed through toxicological studies. Thus, the finding indicates that quince/pectin cross-linked hydrogel sponges are durable enough to deliver the domperidone to the gut for a longer time.

An Insight on Novel Approaches & Perspectives for Gastro-Retentive Drug Delivery Systems.

The conventional oral drug delivery systems face a lot of difficulties in the gastrointestinal tract, such as inappropriate drug release and reduction in the efficacy of the doses, which makes this system less susceptible to the delivery of drug formulation. For the enhancement of therapeutic efficacy and bioavailability of the drug, many efforts have been made. The drug candidates which are not stable at alkaline pH and soluble in acidic medium were selected to increase their therapeutic effectiveness through gastro retentive drug delivery systems (GRDDS). This article discusses various factors which alter the gastro retention time (GRT) of the gastro retentive drug delivery system in the stomach and intestine (duodenum). It emphasizes on the novel approaches made for the delivery and release of drugs with the use of magnetic systems, floating (low-density) systems, super porous hydrogels, raft systems, mucoadhesive systems, high-density systems and expandable systems. Along with the applications, the key aspects of in vivo, in vitro & clinical studies in different approaches to GRDDS have been addressed. In addition, future perspectives have been summarized to reduce gastric transit time in fasting and fed conditions.

A Recent Advantage on Gastroretentive Drug Delivery System: An Overview

In recent years, gastro-retentive drug delivery system (GRDDS) has gained researcher’s interest in the field of oral drug delivery. Various GRDDS approaches can be utilized to retain the dosage forms in the stomach and to release the drug slowly for an extended period of time. GRDDS can be used to prolong the residence time of delivery system in the stomach. This results in targeting of drug release at a specific site for the systemic or local effects. GRDDS can be used to overcome challenges associated with conventional oral dosage forms and to release the drug at a specific absorption site to improve bioavailability of particular drug substance. The challenges include fast gastric emptying of the dosage form which results in the poor bioavailability of the drug. Prolongation of the retention of drugs in stomach those having low solubility at high intestinal pH improves the solubility of drugs. GRDDS has proved to be effective in systemic actions as well as in local actions to treat gastric or duodenal ulcers. Local activity in the upper part of the small intestine can be obtained by improving the residence time of delivery system in the stomach. The system is useful for drugs which are unstable in the intestine or having a low solubility/permeability in the small intestine. Various GRDDS approaches include high density (sinking) systems, low-density (floating systems), muco-adhesive, expandable, unfold able, super porous hydrogel systems, and magnetic systems.

PH-Responsive Super-Porous Hybrid Hydrogels for Gastroretentive Controlled-Release Drug Delivery

Super-porous hydrogels are considered a potential drug delivery network for the sedation of gastric mechanisms with retention windows in the abdomen and upper part of the gastrointestinal tract (GIT). In this study, a novel pH-responsive super-porous hybrid hydrogels (SPHHs) was synthesized from pectin, poly 2-hydroxyethyl methacrylate (2HEMA), and N, N methylene-bis-acrylamide (BIS) via the gas-blowing technique, and then loaded with a selected drug (amoxicillin trihydrate, AT) at pH 5 via an aqueous loading method. The drug-loaded SPHHs-AT carrier demonstrated outstanding (in vitro) gastroretentive drug delivery capability. The study attributed excellent swelling and delayed drug release to acidic conditions at pH 1.2. Moreover, in vitro controlled-release drug delivery systems at different pH values, namely, 1.2 (97.99%) and 7.4 (88%), were studied. These exceptional features of SPHHs-improved elasticity, pH responsivity, and high swelling performance-should be investigated for broader drug delivery applications in the future.

Biodegradable Guar-Gum-Based Super-Porous Matrices for Gastroretentive Controlled Drug Release in the Treatment of Helicobacter pylori: A Proof of Concept.

An increase in resistance to key antibiotics has made the need for novel treatments for the gastric colonization of Helicobacter pylori (H. pylori) a matter of the utmost urgency. Recent studies tackling this topic have focused either on the discovery of new compounds to ameliorate therapeutic regimes (such as vonoprazan) or the synthesis of gastroretentive drug delivery systems (GRDDSs) to improve the pharmacokinetics of oral formulations. The use of semi-interpenetrating polymer networks (semi-IPNs) that can act as super-porous hydrogels for this purpose is proposed in the present work, specifically those displaying low ecological footprint, easy synthesis, self-floating properties, high encapsulation efficiency for drugs such as amoxicillin (AMOX), great mucoadhesiveness, and optimal mechanical strength when exposed to stomach-like fluids. To achieve such systems, biodegradable synthetic copolymers containing acid-labile monomers were prepared and interpenetrated with guar gum (GG) in a one-pot polymerization process based on thiol-ene click reactions. The resulting matrices were characterized by SEM, GPC, TGA, NMR, and rheology studies, and the acidic hydrolysis of the acid-sensitive polymers was also studied. Results confirm that some of the obtained matrices are expected to perform optimally as GRDDSs for the sustained release of active pharmaceutical ingredients at the gastrointestinal level, being a priori facilitated by its disaggregation. Therefore, the optimal performance of these systems is assessed by varying the molar ratio of the labile monomer in the matrices.

A salep biopolymer-based superporous hydrogel for ranitidine delivery: synthesis and characterization

A salep biopolymer-based superporous hydrogel for ranitidine delivery: synthesis and characterization

Superporous hydrogels based on blends of chitosan and polyvinyl alcohol as a carrier for enhanced gastric delivery of resveratrol

Resveratrol exhibits a number of pharmacological properties, notably antioxidant, anti-inflammatory and anti-cancer activities which are beneficial for the treatment of gastric diseases. However, the poor aqueous solubility and rapid metabolism are the important limitations in clinical uses. Superporous hydrogels (SPHs) based on chitosan/PVA blends were developed as a carrier for resveratrol solid dispersion (Res_SD) to increase the solubility and achieve sustained drug release in the stomach. The SPHs were prepared by gas forming method using glyoxal and sodium bicarbonate as cross-linking agent and gas generator, respectively. The solid dispersions of resveratrol with PVP-K30 were prepared by solvent evaporation and incorporated into the superporous hydrogels. All formulations showed rapid absorption of simulated gastric fluid and reached the equilibrium swollen state within a few minutes. The water absorption ratio and mechanical strength of SPHs were predominantly affected by the chitosan content, with maximum values at 1400 % and 375 g/cm2, respectively.The Res_SD-loaded SPHs exhibited good floating properties and SEM micrographs revealed a highly interconnected pores structure with size around 150 μm. Resveratrol was efficiently entrapped within the SPHs at levels between 64 and 90 % w/w and efficient drug release was sustained over 12 h dependent on the concentration of chitosan and PVA. The Res_SD-loaded SPHs exhibited slightly less cytotoxic efffect towards AGS cells than pure resveratrol. Furthermore, the formulation showed similar anti-inflammatory activity against RAW 264.7 cells compared with indomethacin.

Microwave assisted vanillin crosslinked chitosan/polycarbophil superporous hydrogels for biomedical application: Optimization and characterization

Among the numerous macromolecules used in the formulation of superporous hydrogels, naturally occurring polysaccharides like chitosan, alginate, psyllium etc., offer better sustainable building blocks with improved characteristics. Present research work emphasis on development, optimization and characterization of novel superporous hydrogel containing microwave assisted vanillin crosslinked chitosan/polycarbophil (CVP). The preparation of CVP superporous hydrogels was systematically optimized using full factorial design. Optimized CVP superporous hydrogels were subjected for FTIR, DSC and XRD. Residual solvent analysis was performed by gas chromatography. Surface morphology was analysed using SEM. Optimized CVP superporous hydrogel showed good swelling in a pH ranging from 1 to 8 and can be prepared in desired shape and size. FTIR studies revealed the presence of desirable interactions between the polymers. DSC thermograms exhibited differences in comparison to individual polymer thermograms. Residual solvent analysis by gas chromatography method revealed concentration of acetone, in formulation was within permissible limits as per the ICH guidelines. SEM images clearly revealed the formation of the interconnected pores and capillary channels throughout out the formulation. Overall, the current study signifies that the optimized CVP superporous hydrogel formulation can be successfully formulated and employed for regulated delivery of drugs to the GI tract, buccal cavity, colon, vaginal, and rectal region for both local and systemic action for varied therapeutic purposes because of its ability to swell faster in wide range of pH.